This document describes the synthesis and pharmacological evaluation of new benzoxazole derivatives. It first introduces benzoxazoles and their various pharmaceutical and cosmetic uses. It then details the synthesis of a benzoxazole derivative (Compound IV) in a multi-step reaction and provides its structural formula and properties. The document evaluates the acute oral toxicity and analgesic activity of Compound IV in mice based on OECD guidelines. It found that Compound IV had an oral LD50 greater than 2000 mg/kg and showed analgesic effects in the tail immersion test at doses of 50 and 100 mg/kg, suggesting it has potential as a new analgesic drug.
Phenytoin is an anticonvulsant drug or anti-epileptic drug . It can be prepared from the organic compound Benzil, which is formed by the oxidation of Benzoin.
Phenytoin is an anticonvulsant drug or anti-epileptic drug . It can be prepared from the organic compound Benzil, which is formed by the oxidation of Benzoin.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
Biosynthesis and catabolism of acetylcholine. Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.
Parasympathomimetic agents: SAR of Parasympathomimetic agents
Spectrophotometric Determination of Drugs Using Iodine As Analytical ReagentIOSR Journals
Six drugs viz., Astemizole, Cisapride, Domperidone, Pantoprazole, Rabeprazole and Trazadone were tested for the formation of charge transfer complexes with Iodine. Each of these drugs turned the violet coloured i.e iodine , in CH2Cl2, to brown and exhibited a new band at 366nm in addition to the original band of iodine at 510nm due to anion of the reagent whose intensity increased with increase in the concentration of the drugs and formed a basis for quantitative determination of the drugs. The complexes were found to have 1:1 composition and have stability of the order 10 3 to 10 4. The effect of the concentration reagent, polarity of solvent, interference of excipients have been studied and optimized. Dichloroethane (DCE) was found to be suitable solvent for the analysis. The methods have been validated in terms of ICH guidelines and applied to the quantification of pharmaceuticals. The variation of slopes of calibration plots and stability constants of the complexes are discussed in terms of structures of the drugs.
“Synthesis, Characterization, and Antipsychotic Evaluation of Some Aryl Piper...BRNSS Publication Hub
In this proposal research work aryl piperazine derivatives will be synthesised because aryl piperazine currently the most important building blocks in drug discovery with a high number of positive hits encountered in biological screens of this heterocyclic and its congeners. A series N-(4-(benzo[d]thiazol-2-yl)phenyl)-2-[4- (arylsubstituted)piperazines-1-yl]acetamide and N-(4-(benzo[d]oxazol-2-yl)phenyl)-2-[4-(arylsubstituted)piperazines-1-yl]acetamide will be synthesized with different aryl piperzine substituents and their characterization such as melting point determination and Thin layer chromatography (TLC) also performed. After that pharmacological evaluation will be done for synthesized compounds. In pharmacological evaluation the antipsychotic activity determined by behaviour symptoms, Inhibition of 5-hydoxytryptophan (5-HTP) induced head twitches behavior and Induction of catalepsy.
Active constituent of drugs used in diabetic therapyAkshay Kank
In this slide the active constituents which is isolated from herbal sources used for to treat the type 1 and type 2 diabetes is covered. 'Gymnema' and 'swerita chirata' herbal plant is also covered in the slide.This work help in to focus the herbal emphasis on diabetes.
Biosynthesis and catabolism of acetylcholine. Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.
Parasympathomimetic agents: SAR of Parasympathomimetic agents
Spectrophotometric Determination of Drugs Using Iodine As Analytical ReagentIOSR Journals
Six drugs viz., Astemizole, Cisapride, Domperidone, Pantoprazole, Rabeprazole and Trazadone were tested for the formation of charge transfer complexes with Iodine. Each of these drugs turned the violet coloured i.e iodine , in CH2Cl2, to brown and exhibited a new band at 366nm in addition to the original band of iodine at 510nm due to anion of the reagent whose intensity increased with increase in the concentration of the drugs and formed a basis for quantitative determination of the drugs. The complexes were found to have 1:1 composition and have stability of the order 10 3 to 10 4. The effect of the concentration reagent, polarity of solvent, interference of excipients have been studied and optimized. Dichloroethane (DCE) was found to be suitable solvent for the analysis. The methods have been validated in terms of ICH guidelines and applied to the quantification of pharmaceuticals. The variation of slopes of calibration plots and stability constants of the complexes are discussed in terms of structures of the drugs.
“Synthesis, Characterization, and Antipsychotic Evaluation of Some Aryl Piper...BRNSS Publication Hub
In this proposal research work aryl piperazine derivatives will be synthesised because aryl piperazine currently the most important building blocks in drug discovery with a high number of positive hits encountered in biological screens of this heterocyclic and its congeners. A series N-(4-(benzo[d]thiazol-2-yl)phenyl)-2-[4- (arylsubstituted)piperazines-1-yl]acetamide and N-(4-(benzo[d]oxazol-2-yl)phenyl)-2-[4-(arylsubstituted)piperazines-1-yl]acetamide will be synthesized with different aryl piperzine substituents and their characterization such as melting point determination and Thin layer chromatography (TLC) also performed. After that pharmacological evaluation will be done for synthesized compounds. In pharmacological evaluation the antipsychotic activity determined by behaviour symptoms, Inhibition of 5-hydoxytryptophan (5-HTP) induced head twitches behavior and Induction of catalepsy.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
PREPARATION AND IN-VITRO EVALUATION OF ITRACONAZOLE LOADED NANOSPONGES FOR T...Mahewash Sana Pathan
Itraconazole is an imidazole derivative and used for the treatment of local and systemic fungal infections. It is a BCS Class II drug having very low solubility in water i.e. 1-4ng/ml. The oral use of Itraconazole is not much recommended as it has many side effects. The present research has been undertaken with the aim to develop a topical hydrogel formulation of Itraconazole loaded nanosponges to increase the solubility, permeability and stability of itraconazole. Itraconazole loaded nanosponge was prepared by emulsion solvent diffusion method by using different concentrations of ethyl cellulose as a polymer, Polyvinyl alcohol as surfactant and dichloromethane as cross linking agent. Physical characteristics of the nanosponges as well as the drug entrapment efficiency, percentage drug content, Percent yield, drug polymer compatibility, solubility studies of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning electron microscopy of nanosponges showed that they were spherical in shape and spongy in nature. Drug entrapment efficiency was found to be in the range of 42.75 % to 73.10 %. The optimized nanosponge formulation was loaded into hydrogel using carbopol 940 and studied for pH, viscosity, in vitro drug release. Of the nanosponge formulations prepared, F4 was found to show drug release of 70.62%. It was concluded that Itraconazole nanosponge hydrogel may have increased solubility and drug release
Synthesis, Characterization and Biological evaluation of substituted Pyrazole...SriramNagarajan15
The work presented in this article consists of synthesis, characterization and biological evaluation of substituted pyrazole derivatives. Pyrazole derivatives have been shown to have wide variety of pharmacological activities like antimicrobial, antiviral, antihistaminic, antitumor, antipyretic, anti-inflammatory, antidepressant and anticonvulsant. As combination of biologically active moieties into one molecule and synthesis of totally newer moieties have been the methods of research, we present here synthesis of some novel pyrazole derivatives incorporating various biologically active aryl/aryloxy acid derivatives such as ibuprofen, diclofenac, aceclofenac as well as potent antibacterial quinolones, norfloxacin and ciprofloxacin. All the compounds synthesized were evaluated for their antimicrobial activity.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Synthesis and Anti-Inflammatory activity of Sulpha/substituted 1,2-Diazolesinventionjournals
A Novel compound namely N1 (3 Nicotinoyl) 3,5 dimethyl-4-(N-4-sulfamoyl-azo)-1,2-diazoles has been synthesized by two step processes. Synthesis of N1 -4-sulfamoylphenylhydrazono-3,5-dimethyl propane-1,3-dione and sulfonamide, which interacting with 3-Nicotinoyl hydrazine to form final compound. The newly synthesized compound N1 -(3-Nicotinoyl)-3,5-dimethyl 4-(N1 -4-sulfamoyl phenyl azo) 1,2-diazoles was screened for antiinflammatory activity
Synthesis and Anti-Inflammatory activity of Sulpha/substituted 1,2-Diazolesinventionjournals
A Novel compound namely N1 (3 Nicotinoyl) 3,5 dimethyl-4-(N-4-sulfamoyl-azo)-1,2-diazoles has been synthesized by two step processes. Synthesis of N1 -4-sulfamoylphenylhydrazono-3,5-dimethyl propane-1,3-dione and sulfonamide, which interacting with 3-Nicotinoyl hydrazine to form final compound. The newly synthesized compound N1 -(3-Nicotinoyl)-3,5-dimethyl 4-(N1 -4-sulfamoyl phenyl azo) 1,2-diazoles was screened for antiinflammatory activity
Extractive Spectrophotometric Determination of Ulipristal Acetate using Napht...Ratnakaram Venkata Nadh
Ulipristal acetate is used to treat uterine fibroids and for emergency birth control. The present study is a first report on development of a visible spectrophotometric method for determination of Ulipristal acetate present in bulk and tablet formulation. The method involves the sequential addition of HCl (0.1 N) and Napthol Blue Black solution to Ulipristal acetate. Cation formed on tertiary amine group of Ulipristal acetate attracts anion of naphthol blue black (an acid dye) to develop a coloured ion-association complex. From the aqueous phase, the chromophore is extractable into chloroform, which exhibits λmax at 640 nm. As per the existing guidelines of ICH, various parameters of the method were tested for validation. Regression analysis (r > 0.999) shows that the plotted calibration curve exhibits good linearity in the studied range of concentration (2.50 – 15.00 μg mL-1). The % recovery values falls in 99.80 – 100.72 range. %RSD results of both precision studies were observed in the range 0.007 – 0.560, indicating the satisfactory precision of the method. Low values of R.S.D. (< 1 %) were observed indicating that the proposed method is reproducible, accurate and precise. The proposed method can be used in quality control laboratories for routine analysis of Ulipristal acetate (bulk drug and pharmaceutical dosage forms) without requirement of expensive instruments.
Extractive Spectrophotometric Determination of Ulipristal Acetate using Napht...Ratnakaram Venkata Nadh
Ulipristal acetate is used to treat uterine fibroids and for emergency birth control. The present study is a first report on development of a visible spectrophotometric method for determination of Ulipristal acetate present in bulk and tablet formulation. The method involves the sequential addition of HCl (0.1 N) and Napthol Blue Black solution to Ulipristal acetate. Cation formed on tertiary amine group of Ulipristal acetate attracts anion of naphthol blue black (an acid dye) to develop a coloured ion-association complex. From the aqueous phase, the chromophore is extractable into chloroform, which exhibits λmax at 640 nm. As per the existing guidelines of ICH, various parameters of the method were tested for validation. Regression analysis (r > 0.999) shows that the plotted calibration curve exhibits good linearity in the studied range of concentration (2.50 – 15.00 μg mL-1). The % recovery values falls in 99.80 – 100.72 range. %RSD results of both precision studies were observed in the range 0.007 – 0.560, indicating the satisfactory precision of the method. Low values of R.S.D. (< 1 %) were observed indicating that the proposed method is reproducible, accurate and precise. The proposed method can be used in quality control laboratories for routine analysis of Ulipristal acetate (bulk drug and pharmaceutical dosage forms) without requirement of expensive instruments.
Synthesis, Characterization, Biological Evaluation of Some Heterocyclic Oxaze...JohnJulie1
The new serious of pentyloxy and aryloxy benzaldehyde (3ae) were synthesized from the substitution reaction of 4-hydroxy benzaldehyde with different aryl bromide and alkyl bromide, on the basis of Williamson ether synthesis in the presence of Potassium carbonate using absolute ethanol as a solvent. The second step was the synthesis of 2-amino-5-(p-tolyl)1,3,4-thiadiazole.
Synthesis, Characterization, Biological Evaluation of Some Heterocyclic Oxaze...JapaneseJournalofGas
The new serious of pentyloxy and aryloxy benzaldehyde (3ae) were synthesized from the substitution reaction of 4-hydroxy benzaldehyde with different aryl bromide and alkyl bromide, on the basis of Williamson ether synthesis in the presence of Potassium carbonate using absolute ethanol as a solvent. The second step was the synthesis of 2-amino-5-(p-tolyl)1,3,4-thiadiazole.
Design, synthesis, characterization and biological evaluation of 3- (4-(7-chl...iosrjce
Novel thiazolidinone derivatives TQ-VI(1-10) were designed, synthesized and screened for
antimicrobial activity. Synthesis of 3-(4-(7-chloro-2-(4-chlorophenyl) 4-oxo-quinazolin-3(4H)-yl) phenyl) -
2-arylthiazolidin-4-one TQ-VI(1-10) have been achieved from the starting material 2-amino-4-chlorobenzoic
acid TQ-I on cyclization with p-chlorobenzoyl chloride TQ-II to yield 7-chloro-2-(4-chlorophenyl)-4H-3,1-
benzoxazin-4-one,TQ-III, which on treatment with p-phenylindiamine gave 3-(4-aminophenyl)-7-chloro-2-(4-
chlorophenyl)quinazolin-4(3H)-one, TQ-IV in good yield. Then, TQ-IV on reaction with substituted aromatic
aldehydes converted to TQ-V(1-10), which on cyclization with thioglycolic acid gave TQ-VI (1-10). All the
synthesized compounds have been characterized on the basis of IR,
1
H-NMR and mass spectral data. The
compounds containing 4-OH, 4-OCH3 and 3,4,5-(OCH3)3 showed good activity. The title compounds were
screened for qualitative (zone of inhibition) and quantitative antimicrobial activity (MIC) by agar cup plate
method and serial dilution technique, respectively. Among the synthesized compounds in the series, the
compound TQVI4 and TQVI5 were found to exhibit significant antifungal activity at lower concentration of
31.25 µg/ml, against A.niger. The compound TQVI5 and TQVI4 showed zone of inhibition of 17mm and 15mm
against A.niger and C.albicans respectively which is comparable to that of standard drug. The rest of the
analogues in the series displayed weak to moderate antimicrobial activity when compared to the standard
positive controls Ampicillin and Amphotericin B.
Patient compliance: Challenges in management of cardiac diseases in Kuala Lum...pharmaindexing
Background
The objective of this study was to investigate the degree of compliance among cardiac patients who attend the health facilities in Kuala Lumpur and Perak, Malaysia. The reasons for non-compliance and recommendations from healthcare professionals were also evaluated.
Method
A cross-sectional study of 400 patients and 100 healthcare professionals was carried out. This study utilizes variables on external factors and internal factors as the measurement tools. The questionnaire which consists of Morisky self-reported medication adherence questions was administered to patients and causes for non-compliance sought. Questionnaire for healthcare professionals was used to determine strategies that can improve compliance rate.
Results
The study revealed a 15.8% of high adherence rate, 54.3% of moderate adherence rate and 30% of poor adherence to cardiovascular disease medications. The chi-square tests showed the strong association between dependent and independent variables. The model chosen for testing the patient compliance through external and internal factors gives an R2 value of 85.0% with an adjusted R2 of 84.7%. The F value (317.187) was also significant (p=0.000) which means that the variables have better fit in the multivariate model. The major reasons determined for non-adherence were attitudes and beliefs, lifestyle, side effects and cost of medications. The study recommends that pharmacists and dispensing technicians should be adequately qualified to provide proper counselling to cardiac patients on their medicines and disease conditions.
Conclusion
The result of this study is of value to health care providers. Compliance to cardiovascular medications will avoid treatment failures encountered in therapy.
Overview on Recurrence Pregnancy Loss etiology and risk factorspharmaindexing
Recurrent pregnancy loss (RPL) can be defined as more than two to three consecutive miscarriages before 20 weeks’ gestation; it affects approximately 1% to 2% of women. RPL is a multifactorial disease. It is very important to study the etiology and risk factors of RPL to find the best diagnostic tests and suitable therapeutic intervention. This article will discuss the current understanding etiologies and risk factors of RPL.
Novel treatments for asthma: Corticosteroids and other anti-inflammatory agents.pharmaindexing
Asthma management is a challenge due to the prevalence of disease in the world. Based on the immunological and inflammatory mechanisms of asthma, corticosteroids and anti-inflammatory participate greatly in the treatment plan. Due to different reasons, there is still an unmet need to develop new agents in this field. A lot of compounds with anti-inflammatory effect are investigated in both pre-clinical and clinical studies.
A review on liver disorders and screening models of hepatoprotective agentspharmaindexing
The liver is a vital organ present in vertebrates and some other animals. It has a wide range of functions, including detoxification, protein synthesis, and production of bio chemicals necessary for digestion. The liver is necessary for survival; there is currently no way to compensate for the absence of liver function long term, although liver dialysis can be used short term.
Carbamazepine induced Steven Johnson syndrome: A case reportpharmaindexing
Drugs are the most common cause that induces Steven Johnson syndrome (SJS) and includes antiepileptic drugs, antiretroviral drugs, anti-tuberculosis drugs, Sulphonamides, fluoroquinolones, penicillins, non-Steroidal anti-inflammatory drugs, Multivitamins. The genetic markers are also the cause for carbamazepine induced Steven Johnson Syndrome. In our study, the antiepileptic drug (Carbamazepine) is the cause for Steven Johnson Syndrome. A female patient aged 25 years came to the hospital with the complaints of bubbling over the skin and all over the body with papillary vesicles associated with pain and irritation, fever, myalgia, and nausea. The patient is known case of Phenytoin induced Steven Johnson Syndrome. In this case the patient developed the Steven Johnson Syndrome approximately after one month after starting the carbamazepine.By the withdrawal of the drug, the condition of the patient was improved.
Monoherbal formulation development for laxative activitypharmaindexing
The Ayurvedic Pharmacopoeia specifically approves flaxseed as a poultice for boils externally and demulcent or laxative internally. In this study monoherbal formulation development for laxative activity of flaxseed was undertaken. The plantLinumusitatissimumhasshowed higher percentage of total ash as well as alcohol soluble extractive values. The aqueous extract of Linumusitatissimumwas prepared by using pilot scale extraction plant and spray drying unit. The qualitative phytochemical studies reveal the presence of amino acids, carbohydrates, vitamins and proteins. From the available literatures it was found that Linumusitatissimum contains more number of amino acids. The formulated tablets showed acceptable pharmacopoeial limits and complies with specifications for thickness, hardness, friability and weight variation. The formulation has showed better laxative activity indicating additive property of the combined phytoconstituents of the plant.
Monoherbal formulation development for laxative activitypharmaindexing
The Ayurvedic Pharmacopoeia specifically approves flaxseed as a poultice for boils externally and demulcent or laxative internally. In this study monoherbal formulation development for laxative activity of flaxseed was undertaken. The plantLinumusitatissimumhasshowed higher percentage of total ash as well as alcohol soluble extractive values. The aqueous extract of Linumusitatissimumwas prepared by using pilot scale extraction plant and spray drying unit. The qualitative phytochemical studies reveal the presence of amino acids, carbohydrates, vitamins and proteins. From the available literatures it was found that Linumusitatissimum contains more number of amino acids. The formulated tablets showed acceptable pharmacopoeial limits and complies with specifications for thickness, hardness, friability and weight variation. The formulation has showed better laxative activity indicating additive property of the combined phytoconstituents of the plant.
Pneumonia and respiratory failure from swine origin influenza H1n1pharmaindexing
Swine influenza (swine flu) became alarming health concern when World Health Organization declared as “public health emergency of international concern” on April 25, 2009. After documentation of human-to-human transmission of the virus in at least three countries of two WHO regions, the WHO raised the pandemic level to 6.1 During the 1918, flu pandemic infected one-third of the world's population (an estimated 500 million people) and caused approximately 50 million deaths.2 In 1976, an outbreak of swine influenza occurred in New Jersey, USA, which involved more than 200 cases, some of them severe, resulting in one death.3 In 1988, another fatality was reported as a complication of swine influenza.
A descriptive study on newborn care among postnatal mothers in selected mater...pharmaindexing
The newborn health challenge faced by India is more formidable than that experienced by any other country in the world. The newborn health is inevitably affected by the traditional care practices of the mothers causing high infant morbidity and mortality.The aim of the study were determine the knowledge, attitude and practice of postnatal mothers regarding new born care and find out the association between knowledge, attitude and practice of postnatal mothers regarding new born care and to determine the association between these as well as with the selected demographic variables. A descriptive study was conducted to assess the knowledge, attitude and practice of postnatal mothers regarding new born care in selected maternity centres in Madurai. Survey approach was employed to select sample and it consisted of 100 postnatal mothers. Data was collected using structured interview schedule. Findings of the study showed that 65% of postnatal mothers had moderate knowledge; 61% had favourable attitude and 57% of them had high practice of new born care. There was a significant association between knowledge and attitude (r=+0.567), knowledge and practice (r=+0.388), attitude and practice (r=+0.321) .There was a significant association between knowledge and education, monthly family income and obstetrical score at p<0.05. Findings of the study indicated the need to conduct frequent assessment of knowledge, attitude and practice of postnatal mothers regarding new born care. Awareness and attitude of the mothers towards new born care still has lots of lacunae especially in those who belong to the lower socio economic statusand poorly educated postnatal mothers. So it is imperative to provide comprehensive training in the field of new born care for mothers during pregnancy
Late 19th century was evident of intelligent biomaterial; which has changed researcher’s perspective towards science and technology. This intelligent biomaterial are envisioned to have huge impact on Healthcare from sequential signalling of biomedical molecule, mimicking natural gene, an effective drug carrier, to high resolution diagnostic tool.From drug discovery aspect many of NCE fail to reach therapeutic potential due to PK/ PD profile. Nanotechnology has changed the face of drug discovery form chemical evaluation to structure of proteins in signalling pathways and development of chemical antibody. Nanotechnology from lab to market approval is long process due to regulatory evaluation. Though it seems to be bright future market it has to go through a long process from being innovation to complete market product. This makes whole process expensive making investor reluctant to invest in big projects.Western world is aware of dramatic potential of nano-projects; which has its limitation in financial investments; with major challenge of transforming nano science to commercial pharmaceutical product.
The Flaws in health practice in post-operative management of a patient in ter...pharmaindexing
Introduction
Congenital urinary tract obstructions are common cause of kidney damage sometimes which sometimes presents itself without symptoms leading to abnormalities in blood filtration and consequently retarded kidney function. A cohort study was conducted in such patient to find out the short comings in treatment strategy.
Case presentation
A four years old child, weighing 14 kg was brought with severe constipation, fever, chest congestion and cough later developed left eye disorientation after admission to hospital, diagnosed with urinary tract obstruction, indicating acidosis and loss of electrolytes due to excessive loss of water. His therapy management included surgical treatment, dialysis and to improve his electrolyte levels within the normal with the treatment chest congestion and fever.
Conclusion
This case study reports the post operative treatment of congenital urinary tract obstructions in a tertiary care hospital and highlights the discrepancies observed. Antibiotic rationality and irrational prescribing was observed. The case study highlights the need of a clinical pharmacist in the health care team.
Corticosteroid induced disorders – An overviewpharmaindexing
Glucocorticoids are important in the treatment of many inflammatory, allergic, immunologic, and malignant disorders, and the toxicity of glucocorticoids is one of the commonest causes of iatrogenic illness associated with chronic inflammatory disease.Glucocorticoid-induced muscle atrophy is characterized by fast-twitch or type II muscle fiber atrophy. Corticosteroid (CS) therapy is widely used in the treatment of rheumatic diseases.Osteoporosis remains one of its major complications.Steroid induced glaucoma is a form of open angle glaucoma occurring as an adverse effect of corticosteroid therapy. Glucocorticoids induce hepatic and extrahepatic insulin resistance.Glucocorticoid treatment impairs both glucose transport in fat and muscle cells. Corticosteroid-induced psychosis represents a spectrum of psychological changes that can occur at any time during treatment. Cushing’s syndrome describes the signs and symptoms associated with prolonged exposure to inappropriately high levels of the hormone cortisol. Physicians must be aware of these adverse effects and be equipped to manage them.
Anti-inflammatory activity of pupalia lappacea L. Jusspharmaindexing
Pupalia lappacea (L) Juss is an erect shrub used in folklore medicine to treat bone fractures and in inflammatory conditions. Methanolic extract of aerial parts shown is claimed in traditional medicine that the leaves of the plant are used in the treatment of inflammation. In the present study, the methanolic extract of Pupalia lappacea was screened for its anti-inflammatory activity using carageenan induced rat paw edema egg white induced paw oedema models. The methanolic extract at the dose of 200 mg/kg p.o exhibited significant anti-inflammatory activity in carrageenan induced paw edema model (p<0.01). In egg white induced model, methanolic extract at the dose of 200 mg/kg inhibited paw oedema significantly (p<0.01) indicating that both test samples inhibit the increase in number of fibroblasts and synthesis of collagen and mucopolysaccharides during prostaglandin formation during the inflammation. These experimental results have established a pharmacological evidence for the folklore claim of the drug to be used as an anti inflammatory agent. HPTLC analysis of the extract shows the presence of gallic acid 1.24mg/ml, ferulic acid 2.00mg/ml, chlorogenic acid 46.25mg/ml and rutin 7.02mg/ml of the extract which were responsible for the claimed anti-inflammatory action in the animal models studied.
Lucinactant: A new solution in treating neonatal respiratory distress syndrom...pharmaindexing
Lucinactant is a novel synthetic surfactant, approved by the FDA on March 6th 2012, for use in treatment of RDS. It’s superiority as compared to the previously approved surfactants lie in containing sinapultide, a 21-amino acid peptide also known as KL4 peptide, which has been designed to mimic the activity of human surfactant protein. Lucinactant is completely devoid of any animal derived components. It is the fifth drug approved by the FDA for the treatment of RDS. It has shown immense efficacy in phase two clinical trials and animal model studies and exhibited better efficiency when compared to other surfactants in both 24 hour and two week mortality rates of infants in RDS. Lucinactant tends reduce the surface tension at the air-liquid interface of alveolar surfaces and allows lungs to function normally. It was observed that the side effects were lesser with Lucinactant when compared with other naturally derived surfactants.
Bioactivity screening of Soil bacteria against human pathogenspharmaindexing
Microorganisms have a profound effect on medical science as they not only infect & cause disease but also produce metabolic products that can cure infections. Soil happens to be a source for a variety of microorganisms. Most of the bacteria, particularly actinomycetes produce biologically active secondary metabolites. Though there are a number of antibiotics available, there is a pressing need for the discovery of new source for antimicrobials against the pathogens due to the development of drug resistance of the pathogenic microorganisms. In addition to, new pathogenic strains are also developing and causing infection to human beings. Bioactive compounds are compounds that are produced by any living organism and are known to exhibit various biological activities both in-vitro & in-vivo. Bioactivity may be antimicrobial, antineoplastic, anticancerous, immunomodulation, antifertility & others. Soil bacteria were isolated by standard technique and by making use of selective media. The isolates were identified and subjected for preliminary screening to look for their ability to produce bioactive materials. A total of 96 strains were isolated from three different soil samples. 14 of them were found to have antibacterial activity against the human pathogens like Staphylococcus aureus, Streptococcus faecalis, E.coli, Klebsiella aerogenes, Proteus vulgaris, Pseudomonas aureginosa and Salmonella typhi by preliminary screening. Further the selected (3) bacteria were grown in the suitable culture media for the production of bioactive metabolites by using rotary shake flask. The active metabolites was isolated by solvent extraction and concentrated by evaporation under reduced pressure. The antimicrobial screening of the active metabolites showed prominent effect against the clinical pathogens under the study.
A study on sigmoid Volvulus presentation and managementpharmaindexing
A study on sigmoid volvulus presentation and management was a 2yr retrospective study done at RMMCH.The diagnosis of sigmoid volvulus was made from a history of large bowel obstruction (constipation, abdominal distension, and abdominal pain), which were often recurrent and plain abdominal radiographs.The morbidity associated isSuperficial wound infection occurred in four patients. All the infected wounds eventually healed with conservative measures. Clinical anastomotic dehiscence was noted in 1 patient for which during relaparotomy proximal colostomy and mucous fistula was done. The mortality associated is shown is there were 9 deaths of which 7 were due to sepsis and 2 were due to comorbid illness. Two out of eight patients for whom a colopexy was done had a recurrent attack of sigmoid volvulus. The duration of hospital stay ranged between 10 and 21 days. Use of sigmoidoscopic detorsion for viable colon should be encouraged. Sigmoidopexy, which is associated with a recurrence rate of 20% in our series of patients, should be used selectively.Hartmann’s procedure is a safe option in sigmoid volvulus with gangrenous bowel. Primary anastomosis in emergency situation can be carried out with morbidity and mortality in patients with viable colon
Evaluation of Preliminary phytochemical on various some medicinal plantspharmaindexing
The present study was carried out to evaluate the physical status and percentage yield of methanolic extract and its fractions of whole plant of Leucas cephalotes, leaves of Hiptage benghalensis and leaves of Kydia calycina were recorded for future references and Preliminary phytochemical screening of MLC, MHB and MKC revealed the presence of carbohydrates, glycosides, saponins, flavonoids, steroidal and phenolic compounds. MLC revealed the presence of all the above mentioned phytoconstituents except saponins and also MKC steroidal compounds. The fractions of MLC, MHB and MKC revealed the presence of glycosides, phenolic compounds, steroids and flavonoids.
Comparision of in vitro antibacterial activity of cefoperazone and levofloxac...pharmaindexing
Cefoperazone (a third generation cephalosporin) has effective in vitro activity against majority of pathogens. Levofloxacin (a flouroquinolone) is one which prescribed more due to its increased antibacterial activity against Gram-positive, Gram-negative, and atypical bacteria. Microbial resistance to antibiotics is now prevalent and poses a serious clinical threat. An attempt has been made to evaluate sensitivity of Cefoperazone and Levofloxacin against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhi. A total of 120 isolates were collected from different pathological laboratories and medical centers in Karachi, Pakistan. The above stated clinical isolates were extracted from urine/stool, skin, blood and sputum samples. Results show least resistance of Levofloxacin as compare to Cefoperazone against Escherichia coli (32.5% and 42.5%) and Pseudomonas aeruginosa (36% and 48%) while Staphylococcus aureus is still susceptible towards Cefoperazone and least sensitive to Levofloxacin by showing 26.6% and 50% resistance respectively. Study concluded that the prevalent pathogens are still susceptible towards Levofloxacin and Cefoperazone but the gradual increase in resistance is alarming to the general practice of prescribing antibiotic which require routine evaluation and surveillance to ensure the effectiveness of the antibacterial agents.
Concept of srotas from ayurvedic perspective with special reference to neurologypharmaindexing
Ayurveda is a life science. The researchers of ayurveda could rule out the presence of srotas (channels) spreading throughout the human body. These srotas (channels) are governed by vayu which is using all the srotas (channels) of the body to carry out the functional and physiological activities of the human body without which the human society will not exist. Several synonymous words have been described by the ayurvedicacharyas for srotas. Some are micro and some are macro in structures and they adopt the same colour of the particular dhatus of the body to which it belongs. The aim of the study is to justify that srotas are nothing but innurmerable channels or pathways of the nervous system governed by electric current without which no functional and physiological activities of the human body will develope.
Health promotion survey in overweight and obese students of universities in n...pharmaindexing
Introduction
Overweight and obesity is one of the major health problems in the UK and worldwide. Approximately two-thirds of the population in the UK is either overweight or obese. Overweight and obesity is an important issue that causes distress to most women. Health promotion is the best method to educate overweight and obese women. It is defined as the process enabling people to increase control over and to improve their health by Ottawa Charter for Health Promotion. It is aimed to enhance the well-being of the individuals and their positive attitudes towards prevention of various diseases. In order to make any improvement to the health promotion for overweight and obesity, the risk factors and the opinions from the public should first be identified and addressed.
Methods
Cross-sectional survey design was selected with a questionnaire that consisted of 20 open and close ended questions. A sample size of 196 was determined. The data thus gathered was analyzed using SPSS V20 (Statistical Package for Social Science version 20). Descriptive statistics (fx) and (SD) were used and Chi-square X2 test for association was employed.
Results
Out of the total 196 responses, only (40%) of the students had normal weight (SD 1.1), (25%) students had a good understanding of health promotion (SD 1.6), half (50%) appeared concerned about their weight (SD 0.5), (60%) had an obese family member (0.5). The BMI of students was associated with the presence of an obese member in their family and their weight as a concern for them. (P-value <0.05).
Conclusion
The health promotion service is beneficial as it was found to have raised concerns in the mind of the students regarding over weight and obesity. However it was observed that the understanding of health promotion service was different among students and this is the root of the problem.
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
Acute scrotum is a general term referring to an emergency condition affecting the contents or the wall of the scrotum.
There are a number of conditions that present acutely, predominantly with pain and/or swelling
A careful and detailed history and examination, and in some cases, investigations allow differentiation between these diagnoses. A prompt diagnosis is essential as the patient may require urgent surgical intervention
Testicular torsion refers to twisting of the spermatic cord, causing ischaemia of the testicle.
Testicular torsion results from inadequate fixation of the testis to the tunica vaginalis producing ischemia from reduced arterial inflow and venous outflow obstruction.
The prevalence of testicular torsion in adult patients hospitalized with acute scrotal pain is approximately 25 to 50 percent
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
Knee anatomy and clinical tests 2024.pdfvimalpl1234
This includes all relevant anatomy and clinical tests compiled from standard textbooks, Campbell,netter etc..It is comprehensive and best suited for orthopaedicians and orthopaedic residents.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Synthesis and Pharmacological evaluation of new Benzoxozole Derivatives
1. 59
* Corresponding author: G.Kalyani
E-mail address: kallukln477@gmail.com
IJPAR |Volume 2 | Issue 2 | Apr - Jun- 2013 ISSN: 2320-2831
Available Online at: www.ijpar.com
[Research article]
SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NEW
BENZOXOZOLE DERIVATIVES
*1
G.Kalyani, 2
Raju Bathula, 3
B.Vinatha, 4
Perka Harathi,5
K.Ramadevi
1,3,4
Department of Pharmaceutical Chemistry,TKR College Pharmacy, JNTU, Hyderabad,
Andrapradesh, India.
2
Department of Pharmaceutical Chemistry, Avanthi Institute of Pharmaceutical Sciences,
JNTU, Hyderabad, Andrapradesh, India.
5
Department of Chemistry, Osmania University, Hyderabad, Andhra Pradesh, India.
ABSTRACT
Benzoxazoles1
are usually prepared by heating 2-Aminophenol with formic acids in the presence of Boric
acid under reflux. Condensation of these two substances under milder conditions. Being a heterocyclic
compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive
structures. It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen.
Benzoxazole derivatives are provided a protection against noxious UV radiation.Benzoxazole derivatives are
also used in cosmotic compositions, such as for examples mainly cinnamic acid, 4-aminobenzoic
acid.Benzoxazole derivatives are also used in the optical brighteners.These derivatives are used as
Anticonvulsant and Neurotoxicity2
, Anti-inflammatory agents3
, “Antibacterial activity”4
, Cholesteryl ester
transfer Protein inhibitors5
, Antimicrobial activity6,7
, Antifungal activity’8
, Cyclooxygenase inhibitors9
, hair
treatment products and also used as a skin protectants.
Key words: Inflammatory agents, Antibacterial activity, Benzoxazole, cinnamic acid, 4-aminobenzoic acid,
optical brighteners.
INTRODUCTION
Being a heterocyclic compound, benzoxazole finds
use in research as a starting material for the
synthesis of larger, usually bioactive structures. It
is found within the chemical structures of
pharmaceutical drugs such as flunoxaprofen.
Benzoxazole derivatives are provided a protection
against noxious UV radiation.Benzoxazole
derivatives are also used in cosmotic
compositions, such as for examples mainly
cinnamic acid, 4-aminobenzoic acid.
Cyclooxygenase (COX; prostaglandinendoperoxide
synthase) metabolizes Arachidonic acid to
Prostaglandin (PG) H2, which serves as the
precursor for the biosynthesis of various PGs,
Thromboxanes, and Prostacyclin.COX activity
originates from two distinct and independently
regulated isozymes, COX-1 and COX-2.COX-1 is
a constitutive enzyme, whereas COX-2 is
inducible and short-lived. COX-2 is the product
of an immediate-early gene, and is stimulated
by a host of growth factors, cytokines, and
mitogens.
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Its expressionCOX-1 appears responsible for the
biosynthesis of PGs in the gastric mucosa and
in the kidney, whereas COX-2 appears
responsible for biosynthesis in inflammatory
cells and the central nervous system.Non-steroidal
anti-inflammatory drugs (NSAIDs) inhibit the
two isoforms to different extents, and this
feature accounts for their shared therapeutic
properties and side effects.The differential tissue
distribution of the COX isozymes has provided
a rationale for the development of COX-2-
selective inhibitors as non-ulcerogenic, anti-
inflammatory, and analgesic agents.Most selective
COX-2 inhibitors, including the recently
approved drugs celecoxib and rofecoxib belong
to the diaryl heterocycle class of compounds.
MATERIALS
Glassware is of Borosilicate grade. Melting point
apparatus, TLC on silica gel-G plate, KBr on a
THERMONICOLATE NEXUS-670 sprectro
photo meter, DMSO – d6 with TMS as internal
standard, 2-Aminophenol, Chloro acetic acid
(0.1mole), methanol .
METHOD
All the chemicals were obtained from S.D. Fine
chem. Limited mumbai all the glassware is of
Borosilicate grade . Melting points were
determined in open capillaries and are uncorrected.
The purity of the compound was ascertained by
TLC on silica gel-G plate. Characterization of
synthesized compound was done by spectral
studies. IR spectra were taken in KBr on a
THERMONICOLATE NEXUS-670 sprectro
photo meter. 1
H NMR spectra was recorded on
brucker avance 300 MHZ spectrophoto meter in
DMSO – d6 with TMS as internal standard. The
chemical shift values are in delta (ppm). Physical
data and Analgesic activities of synthesized
compound was recorded in table .
SYNTHESIS OF 3-[(BENZOOXAZOLE-
2-YL METHYL) - AMINO]-2-(4-NITRO
PHENYL) -THIOZOLIDINE -4-ONE
SYNTHESIS OF 2-CHLORO METHYL
BENZOXAZOLE (I)
2-Aminophenol (0.1mole) is taken into a clean
250ml of RBF flask and it is fixed to the
condenser and add Chloro aceticacid(0.1mole) in
excess under reflux for 2 hours. The reaction
mixture was cooled in ice water. The product thus
separated with filtered and washed with cold
water. The product was recrystallized by methanol
as a solvent.(M.P – 610
C ; Product Yield – 72%)
SYNTHESIS OF BENZOOXAZOLE 2-YL-
METHYL HYDRAZINE (II)
2-Chloro methyl benzoxazole (0.01mole) in
ethanol is refluxed with Hydrazine hydrate
(0.01mole) for 6 hours. After the reaction mixture
was taken into a china dish and it was kept on a
flame after few minutes pink, cream like solid
mass was appeared after it was cooled for few
minutes a light pink solid mass appeared. This is
recrystallized from ethanol to get the desired
compound as a solid.(M.p – 750
C ; Product yield –
78%)
SYNTHESIS OF N-BENZOOXAZOLE-2-YL
METHYL-N-(4-NITRO-BENZYLIDENE)-
HYDRAZINE (III)
Benzooxazole-2-yl-methyl hydrazine (0.01mole) in
ethanol is refluxed with 4-Nitro Benzaldehyde
(0.01mole) for 10 hours. After the mixture was
taken into a beaker and it was kept in a ice cold
water, a yellow solid mass separated. This crude
product is recrystallized from ethanol to get
desired product as solid. (M.p – 930
C ; Product
yield – 69%)
SYNTHESIS OF 3-[(BENZOOXAZOLE-2-
YLMETHYL)-AMINO]-2-(4-NITRO
PHENYL)-THIOZOLIDINE-4-ONE (IV)
0.01mole of N-Benzooxazole-2-yl-methyl-N-(4-
nitro-benzylidene)-hydrazine is dissolved/soluble
in dry benzene and to this (0.01mole) of
thioglycolic acid is added. A pinch of fussed zinc
chloride is added to the reaction mixture. The
reaction mixture is then refluxed for 10hours.
The removal of benzene is carried out using the
dean stark water separator till no more water
separated with benzene.i.e. The turbidity of
benzene is removed. The excess of benzene
removed by vacuum distillation. The above mixture
is then cooled to room temperature and poured into
a beaker containing ice cold water.
The reaction mixture is then treated with ice-cold
water containing sodium bicarbonate (NaHCO3) to
remove the unreacted thioglycolic acid. The
separated product is then recrystallized from
absolute ethanol to yield.
(M.p – 1030
C ; Product yield – 71%)
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SCHEME
NH2
OH
+
Cl
OH
O
2-aminophenol
chloroacetic acid
cyclization N
O
Cl
2-(chloromethyl)-1,3-benzoxazole
NH 2.NH 2.H2O
N
O NH NH2
2-(hydrazinylmethyl)-1,3-benzoxazole
-HCL
N
O NH N
N
+
O
-
O
N
+
O
-
O
O
4-nitrobenzaldehyde
2-{[2-(4-nitrobenzylidene)hydrazinyl]methyl}-1,3-benzoxazole
SH
OH
O
sulfanylacetic acid
-H2O
N
O NH
N
S
O
N
+
O
-
O
3-[(BENZOOXAZOLE-2-YL METHYL)-AMINO]-2-(4-NITRO PHENYL)-
THIOZOLIDINE-4-ONE (IV)
-H2O
(III)
(II)
(I)
Physical data of Synthesized compound (IV)
Compound Structure M.P
(0
C)
Yield
(%)
Molecular
Formula
IV
O
N
CH2NH N
S
O
NO2
3-[(Benzooxazol-2-ylmethyl)-amino]-2-(4-nitro-phenyl)-thiazolidin-4-one
103 71 C17H14N4O4S
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BIOLOGICAL EVALUATION
Invivo biological evaluation
Materials and methods
The various animals and materials used for the
present study and their sources are as follows.
a) Swiss albino mice
b) 1% of carboxy methyl cellulose (Rolex
laboratories)
c) Pentazocin (Fortwin)
d) Water for injection
e) Synthesized compound
f) Hot plate
The animals used in the present study such as
swiss albino mice weighing 20-50gm was kept
in colony cage at 25 ± 20
C, relative humidity of
45-55% under 12hrs light and dark cycle. The
animal was feed with standard animal feed and
water ad libitum. The test compound was
administered orally using intragastric tube in
the form of suspension using 1% CMC as
suspending agent. The experimental dose was
selected between the minimum effective dose
and maximal non lethal dose.
ANOVA followed by dunnets “t” test was
performed to ascertain the significance of the
exhibited analgesic activity of the synthesized
compound.
Acute oral toxicity ( Acute toxic class
method in mice)
Analgesic activity ( Tail – Immersion method
in mice)
Evaluation of Acute oral Toxicity
Introduction
Acute oral toxicity defines to dose adverse
effects occurring following oral administration
of a single dose of substances or multiple
doses given within 24 hrs. The various methods
used to evaluate the acute oral toxicity are as
follows.
Fixed dose procedure (OECD guideline-420)
Acute toxic class methods (OECD guideline-423)
Ups and down Procedure (OECD guideline-425)
OECD guideline-423
OECD guidelines for the testing of chemicals
are periodically reviewed in the light of
scientific progress or changing as the second
alternative to the conventional acute toxicity
test, described in the test guideline 401.
Experimental protocol (Acute toxic class
method in mice)
In the present study the acute oral toxicity of
the synthesized compound was performed by
acute toxic class method. In this methods the
toxicity of the synthesized compound was
tested using a step wise procedure, each step
using three mice of a single sex. The mice
were fasted prior to dosing (food but not water
should be with held) for 3-4 hrs.
Following the period of fasting the animal
should be weighed and the synthesized
compound is administered orally at a dose of
2000 mg/kg body weight. Animals were
observed individually after dosing atleast once
during the first 30 minutes; periodically during
the first 24 hrs with special attention given
during the first 4 hrs and daily thereafter, for
a total of 14 days. As know mortality was
observed with the above dose. So, a series of doses
50 and 100 mg/kg body weight were selected
for the further pharmacological evaluation. The
test procedure with a starting dose of
2000mg/kg body weight as per OECD-423
guidelines.
Evaluation of Invivo Analgesic activity
Introduction
Pain is unpleasant sensory and emotional
experience associated with actual or potential
tissue damage is described in terms of such
damage. Analgesics are substances which
relieve or decrease pain sensation by increasing
threshold to pain full stimuli without causing
loss of consciousness. Analgesics can be
evaluated in three different ways as follows.
a) Prevention or relief of artificially induced
pain in experimental animals.
b) Relief of experimental pain in human
volunteers and
c) Relief of pathological or incisional pain in
patients.
In human beings, the analgesics are evaluated
either against experimentally induced pain
(Radiant heat, ischemia induced with
sphygmomanometer cuff , intra peritoneal
bradikinin) or against endogenous pain (post-
puerperal pain , post operative pain and pain due
to malignancy).
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In animals painfull reaction can be artificially
induced by the any one following methods.
Thermal method (Radiant heat as a source
of pain)
Chemical method (Irritants such as acetic
acid &bradykinin)
Physical pressure method (Tail compression).
Experimental protocol 10 (Tail immersion
method in mice)
The analgesic activity was determined by tail-
immersion method. Swiss mice (n=6) of either
sex selected by random sampling technique
was used for the study. Pentazocine at the
dose of 10mg/kg (i.p.) was administered as
standard drug for comparison the test
compounds at dose level 50 & 100 mg/kg were
administered orally. The animals were held in
position by a suitable restrainer with the tail
extending out and the tail (up to 5cm) was
taken dipped in a beaker of water maintained at
55±0.50
C. The time in sec taken to withdraw
the tail clearly out of water was taken as
reaction time. The first reading (0 min) was
taken immediately after the administration of
the test compound and subsequent reaction time
was recorded at 30,60,120 & 180 min after the
administration of compound. A cut off point of
15 sec was observed to prevent the tail
damage. The percentage analgesic activity was
calculated using the following the formula and
results are presented in table no 7.2.
PAA = [(T2-T1)/T2]×100
Where,
T1 is the reaction time (in sec) before treatment.
T2 is the reaction time (in sec) after treatment.
PAA is the percentage analgesic activity.
RESULTS & DISCUSSION
Acute oral toxicity study of synthesized
compound
Acute oral toxicity studies were performed
according to the OECD guideline 423 method.
This method has been designed to the
evaluate the substance at the fixed doses
and providing information both for hazard
assessment and substance to the ranked for
hazard classification purpose.
The synthesized compounds were
administered initially at a starting dose of
2000mg/kg b.w. in 1% CMC (p.o.) and
observed 14 days mortality due to acute
toxicity.
Careful observation were made at least
twice a day for the effect on CNS , ANS ,
motor activity salivation, skin coloration and
other general signs of toxicity were also
observed and recorded.
Since no sign of toxicity observed at
2000mg/kg b.w. to the group of animals ,
the LD50 value of the title compounds
expected to exceed 2000mg/kg b.w. and
represented as class 5.
(2000mg/kg < LD50<2500mg/kg)
From the toxicity studies the data revealed
that all the synthesized compounds proved
to be non toxic at tested dose levels and
well tolerated by the experimental animals
as their LD50 cut of values less than
2000mg/kg b.w.
Invivo Analgesic Activity of the Synthesized
Compound
Synthesized Compound was evaluated for
Analgesic activity by Tail Immersion method.
The activity was studied at 50mg/kg , 100mg/kg
b.w (p.o) and their effects were measured at
the time interval of 30, 60,120 and 180 minutes.
Synthesized compound showed significant
analgesic activity. Heighest analgesic activity was
observed at 120 minutes for the compound
(100mg/kg).
When compared with standard drug
(Pentazocin 10mg/kg) the compound exhibited
comparable analgesic activity at 100mg/kg b.w
6. 64
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180min
%
27.92
57.52
70.10
-------
MEAN±
SEM
6.17±0.31
NS
6.67±0.42
*
8.46±0.20
**
3.19±0.10
120min
%
44.02
77.98
80
-------
MEAN±
SEM
7.33±0.42
*
8.33±0.42
**
8.47±0.23
5**
3.27±0.09
60min
%
50.06
71.18
80.10
------
MEAN±
SEM
6.67±0.33
*
7.17±0.40
*
8.46±0.20
1**
3.31±0.19
30min
%
41.07
68.27
78.10
------
MEAN±
SEM
5.50±0.43
NS
5.67±0.33
*
8.2±0.31**
3.32±0.26
0min
MEAN±
SEM
3.83±0.40
3.50±0.34
3.35±0.19
3.31±0.2
Dose
(mg/kg)
50
100
10
2ml
(1%CMC)
0
Compounds
IV
IV
STD
(Pentazocin)
Control
AnalgesicactivitydataoftheSynthesizedcompound
7. 65
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I.R. Spectra data of synthesized
compound
The synthesized compound of the present study
was characterized through IR spectra. The
synthesized compound of the present study
showed characteristic absoption bands for -
NO2-, -S-CH2-CO, HN-CH2-C, N-CH-S, Ar-H
groups.
S.NO Functional groups Wave number(cm-1
)
1. NO2 (1307-1610 cm-1
) 1519.67
2. -N-CO-CH2 (600-700 cm-1
) 686.72
3. HN-CH2-C (1600-1710cm-1
) 1705.19
4. N-CH-S (700-1563cm-1
) 1347.76
5. S-C-CO (2300-3060 cm-1
) 2919.52
C:Program FilesOPUS_65MEASbenzoxazole.0 benzoxazole Instrument type and / o 23/04/2012
2919.52
2851.09
2558.50
1705.19
1593.85
1519.67
1347.76
1296.40
1197.88
1156.82
1111.08
1015.80
938.84
860.89
723.49
686.72
665.71
100015002000250030003500
Wavenumber cm-1
707580859095100
Transmittance[%]
Page 1/1
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1
H NMR. Spectral data of synthesized
compound
The synthesized compound of the present
study was characterized through 1
H NMR
spectra. The synthesized compound of the
present study showed characteristic absoption
bands for -NH-, -S-CH2-CO, HN-CH2-C, N-CH-
S, Ar-H groups.
S.NO Proton type ᵟ
1. -NH- 2.5 (s)
2. -S-CH2-CO 3.3 (s)
3. HN-CH2-C 3.45 (s)
4. N-CH-S 5.5 (s)
5. Ar-H 7.6-7.8 (s)
6. Ar-H 8.2-8.4 (d)
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SUMMARY AND CONCLUSION
The thesis deals with the synthesis and
biological evaluation of novel benzoxazole
derivatives. The synthesized compound was
characterized by IR & 1H NMR.
The thesis deals with the introduction of
therapeutic agent based on Benzoxazole moiety,
Literature survey on the investigation carried
out by the earlier workers in the synthesis and
biological evaluation of novel benzoxazole
derivatives, Aims & objectives, Plan of work,
Experimental work including detailed procedure
for synthesis of title compounds and Physical
data of synthesized compounds containing
molecular formula, melting point, percentage of
yield finally describes results of experimental
investigations and discussion of results.
Synthesized compound was evaluated for analgesic
activity by tail-immersion method. The activity
was observed at 50 mg/kg &100mg/kg b.w. (p.o)
and their effects were measured at the time
interval of 30, 60, 120 and 180 minutes.
The synthesized compound (IV) was found at
100 mg/kg b.w. dose “t” Significant analgesic
activity in all the cell lines.
Finally for the development of better
therapeutic agent for clinical assessment,
detailed pharmacology and toxicology studies
need to be performed in order to generate data
on the potential short and long – term toxicities
as well as affirmed pharmacological action. The
discovery and the applications of such synthetic
drugs will play a role in human as well as
veterinary medicine in the future.
BIBILOGRAPHY
[1] Raj k. Bansal. Heterocyclic chemistry, 4(2008) page.no : 470-474
[2] NadeemSiddiqui et al., Pharm.sciences, Polish pharmaceutical society (2008).
[3] Sunila T. Patil et al., International Journal of Pharma. Research & Development (2010) 0974-9446.
[4] Jong Yeon Hwang et al., J.Comb.Chem.(2006)
[5] Mukeshyadav et al., Journal of drug discovery (2011).
[6] Dr.SrinivasAmpati et al., International Journal of Pharma. Research & Development (2010) 0974-9446.
[7] L.Srikanth, Ushanaik et al., International Journal of Pharma and Bio sciences.(2010)
[8] EsinSener (1997) et al., Journal of Pharma and Bio sciences (2010).
[9] Srinivas Ampati et al., PharmaChemica (2010).
[10]Srivastava Ashok .k. Bahel suresh c., J.Indian.Chem soc.,53 (8), 1976, PP- 841.
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