Anti Malarial Drugs of medicinal chemistryPranjal Saxena
This slide contain information about Anti Malarial Drugs and their description with the synthesis of Chloroquine and pamaquine
SAR of quinolines
Miscellaneous agents of anti Malarial
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
Anti Malarial Drugs of medicinal chemistryPranjal Saxena
This slide contain information about Anti Malarial Drugs and their description with the synthesis of Chloroquine and pamaquine
SAR of quinolines
Miscellaneous agents of anti Malarial
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
Sulfonamide (also called sulphonamide, sulfa drugs or sulpha drugs) is the basis of several groups of drugs. The original antibacterial sulfonamides are synthetic antimicrobial agents that contain the sulfonamide group.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
Malignancy is most familiar as a characterization of cancer.Chemotherapy is a category of cancer treatment that uses one or more anti-cancer drugs as part of a standardized chemotherapy regimen
lead optimization of macrolide drug about
Contents
Introduction
MOA of Antibiotic
Macrolides- General Consideration
Mechanism of Action of Macrolide Antibiotics
Inhibition Of Protein Synthesis
Chemistry of Macrolides
Classification of Macrolide Antibiotics
Structure Activity Relationship
Lead Optimization
Structure of Macrolide Drug
Roxithromycin
Erythromycin
Macrolide Indications
Sulfonamide (also called sulphonamide, sulfa drugs or sulpha drugs) is the basis of several groups of drugs. The original antibacterial sulfonamides are synthetic antimicrobial agents that contain the sulfonamide group.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
Malignancy is most familiar as a characterization of cancer.Chemotherapy is a category of cancer treatment that uses one or more anti-cancer drugs as part of a standardized chemotherapy regimen
lead optimization of macrolide drug about
Contents
Introduction
MOA of Antibiotic
Macrolides- General Consideration
Mechanism of Action of Macrolide Antibiotics
Inhibition Of Protein Synthesis
Chemistry of Macrolides
Classification of Macrolide Antibiotics
Structure Activity Relationship
Lead Optimization
Structure of Macrolide Drug
Roxithromycin
Erythromycin
Macrolide Indications
macrolides antibiotics .Macrolidele, o clasă de antibiotice bine-cunoscută, sunt inițial izolate din Streptomyces erythreusîn anii 1950. Macrolidele sunt inhibitori puternici ai sintezei proteinelor , prin legarea la subunitatea ribozomală 50S a bacteriilor la centrul peptidil transferazei format de ARNr 23S. Studiile au sugerat că blochează și formarea subunității 50S în celulele în creștere. Macrolidele ar putea, prin urmare, să adauge un nou mecanism de acțiune la terapia combinată a TB și, prin urmare, ar putea, de asemenea, să dețină promisiunea de a fi la fel de eficiente împotriva MDR-TB și a TB sensibilă la medicamente. Macrolidele, cunoscute ca fiind active oral, s-au dovedit, de asemenea, a fi sigure și bine tolerate atunci când sunt utilizate pentru indicații non-TB. Cheie pentru tratamentul tuberculozei, macrolidele tind să prezinte niveluri ridicate de activitate intracelulară și o distribuție extinsă în plămâni. Macrolidele s-au dovedit deja a fi utile clinic în tratamentul altor boli micobacteriene, inclusiv MAC și lepra.Antibioticele macrolide sunt o clasă importantă de antibiotice active pe cale orală. 18 Figura 4Membrii majori ai clasei includ eritromicină și azitromicină , precum și telitromicină , care a fost aprobată în 2004 ( ). Macrolidele sunt utilizate cel mai frecvent împotriva organismelor Gram-pozitive, deoarece sunt slab active împotriva majorității bacililor Gram-negativi. Macrolidele sunt în general agenți bacteriostatici care se leagă de ARNr -ul 23S de pe subunitatea mare și blochează „tunelul” prin care iese lanțul peptidic în creștere. Rezistența la macrolide apare dintr-o metilază care modifică ținta ribozomală și reduce legarea, împreună cu enzimele care modifică chimic structurile medicamentului și mecanisme mai generale de rezistență la absorbție/eflux. Spre deosebire de aminoglicozide , macrolidele sunt în general bine tolerate și dau naștere la câteva probleme grave de toxicitate și, ca atare, sunt utilizate pe scară largă.
Enzimele implicate în modificarea ribozomului sunt produse în mod inductibil sau constitutiv (38) și sunt codificate de o clasă de gene numite erm (metilarea ribozomului eritromicină) (36-39) . Aproximativ 30 de gene erm au fost izolate și caracterizate dintr-o varietate de organisme care sunt rezistente clinic la eritromicină, dintre care cea mai răspândită este ermC (36,37,40-42) gena erm (43). Atât în bacteriile gram-pozitive și gram-negative care poartă gena, metilarea unui anumit reziduu de adenină într-o regiune foarte conservată a ARNr 23S a fost implicată în rezistența la MLS . Acest reziduu se află într-o regiune a ribozomului direct implicată în formarea centrului peptidil transferazei și, la metilare, conferă rezistență la toate macrolidele, lincosamidele și antibioticele din clasa B cunoscute de streptogramină.
Deoarece rezistența la MLS este direct legată de genotipul erm (4,15) . O astfel de abordare a fost întreprinsă recent pentru a identifica compuși care ar inhiba
Macrolides are a class of antibiotics derived from Saccharopolyspora erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.
Macrolides act by binding to bacterial 50S ribosomal subunit and inhibit protein synthesis in bactera. Chemistry with examples Erythromycin, Roxitromycin, azithromycin, Clarithromycin.... Mechanism of action and side effects....
Chemical products clarithromycin descriptionhuenumb
Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor.Target: Antibacterial; CYP3A4Clarithromycin is a macrolide antibiotic used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydophila pneumoniae), skin and skin structure infections. Clarithromycin prevents bacteria from growing by interfering with their protein synthesis. It binds to the subunit 50S
Pharmacy Practice
Scope of pharmacy practice
Community Pharmacy
Scope of community pharmacy
Community pharmacy management
Selection of Pharmacy site
Objective
Legal requirements
Drug procurement
Drug storage and inventory control
Pharmacy Practice is the discipline of pharmacy which involves developing the professional roles of pharmacists. Pharmacy Practice offers practicing pharmacists in-depth useful reviews and research trials and surveys of new drugs and novel therapeutic approaches.
Books
A book is a set of written, printed, illustrated, or blank sheets, made of ink, paper, parchment, or
other materials, usually fastened together to hinge at one side. A single sheet within a book is
called a leaf, and each side of a leaf is called a page.
Books may also refer to works of literature, or a main division of such a work. In library and
information science, a book is called a monograph, to distinguish it from serial periodicals such
as magazines, journals or newspapers. The body of all written works including books is
literature. In novel sand sometimes other types of books (for example, biographies), a book may
be divided into several large sections, also called books.
Text Books
A textbook or course book (UK English) is a manual of instruction in any branch of study.
Textbooks are produced according to the demands of educational institutions. Schoolbooks are
textbooks and other books used in schools. Although most textbooks are only published in
printed format, many are now available as online electronic books
Another name of anti-body is immunoglobulins . Anti-body is the glycoprotein which is produce by Bcell and which are responsible to bind antigen with higher specifity and affinity. Anti-body is mainly
distrusted in body fluid and also present surface of some cell.
Polycyclic aromatic hydrocarbons (PAHs, also polyaromatic hydrocarbons) are hydrocarboz—
organic compounds containing only carbon and hydrogen—that are composed of
multiple aromatic rings (organic rings in which the electrons are delocalized). Formally, the class
is further defined as lacking further branching substituents on these ring structures. Polynuclear
aromatic hydrocarbons (PNAs) are a subset of PAHs that have fused aromatic rings, that is, rings
that share one or more sides.
The simplest such chemicals arenaphthalene, having two aromatic
rings, and the three-ring compounds anthracene and phenanthrene.
It is a health specialty, which describes the activities and services of the clinical pharmacist to develop and promote the rational and appropriate use of medicinal products and devices.
Clinical Pharmacy includes all the services performed by pharmacists practising in hospitals, community pharmacies, nursing homes, home-based care services, clinics and any other setting where medicines are prescribed and used.
The term "clinical" does not necessarily imply an activity implemented in a hospital setting. It describes that the type of activity is related to the health of the patient(s). This implies that community pharmacists and hospital pharmacists both can perform clinical pharmacy activities
Generate greater customer satisfaction
• Create savings
• To identify strategic opportunities and niches
• Increase marketing effectiveness
• Allocation of marketing budget
• Adjustment of product to the market need
• To estimate the level of sales in the market
• To overcome competition effectively
• To develop effective marketing programmers
• To contribute towards achieving company goals
• To develop marketing activities
POSITIONING
COMPONENTS OF POSITIONING
MARKET POSITIONING MAP
5 EASY STEPS FOR BRAND POSITIONING
REAL EXAMPLES OF MARKET POSITIONING MAP
TYPES OF MARKET POSITIONING
PRODUCT POSITIONING PROCESS
APPROCHAES TO POSITIONING STRATEGY
Introduction to AI for Nonprofits with Tapp NetworkTechSoup
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Francesca Gottschalk - How can education support child empowerment.pptxEduSkills OECD
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June 3, 2024 Anti-Semitism Letter Sent to MIT President Kornbluth and MIT Cor...Levi Shapiro
Letter from the Congress of the United States regarding Anti-Semitism sent June 3rd to MIT President Sally Kornbluth, MIT Corp Chair, Mark Gorenberg
Dear Dr. Kornbluth and Mr. Gorenberg,
The US House of Representatives is deeply concerned by ongoing and pervasive acts of antisemitic
harassment and intimidation at the Massachusetts Institute of Technology (MIT). Failing to act decisively to ensure a safe learning environment for all students would be a grave dereliction of your responsibilities as President of MIT and Chair of the MIT Corporation.
This Congress will not stand idly by and allow an environment hostile to Jewish students to persist. The House believes that your institution is in violation of Title VI of the Civil Rights Act, and the inability or
unwillingness to rectify this violation through action requires accountability.
Postsecondary education is a unique opportunity for students to learn and have their ideas and beliefs challenged. However, universities receiving hundreds of millions of federal funds annually have denied
students that opportunity and have been hijacked to become venues for the promotion of terrorism, antisemitic harassment and intimidation, unlawful encampments, and in some cases, assaults and riots.
The House of Representatives will not countenance the use of federal funds to indoctrinate students into hateful, antisemitic, anti-American supporters of terrorism. Investigations into campus antisemitism by the Committee on Education and the Workforce and the Committee on Ways and Means have been expanded into a Congress-wide probe across all relevant jurisdictions to address this national crisis. The undersigned Committees will conduct oversight into the use of federal funds at MIT and its learning environment under authorities granted to each Committee.
• The Committee on Education and the Workforce has been investigating your institution since December 7, 2023. The Committee has broad jurisdiction over postsecondary education, including its compliance with Title VI of the Civil Rights Act, campus safety concerns over disruptions to the learning environment, and the awarding of federal student aid under the Higher Education Act.
• The Committee on Oversight and Accountability is investigating the sources of funding and other support flowing to groups espousing pro-Hamas propaganda and engaged in antisemitic harassment and intimidation of students. The Committee on Oversight and Accountability is the principal oversight committee of the US House of Representatives and has broad authority to investigate “any matter” at “any time” under House Rule X.
• The Committee on Ways and Means has been investigating several universities since November 15, 2023, when the Committee held a hearing entitled From Ivory Towers to Dark Corners: Investigating the Nexus Between Antisemitism, Tax-Exempt Universities, and Terror Financing. The Committee followed the hearing with letters to those institutions on January 10, 202
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Welcome to TechSoup New Member Orientation and Q&A (May 2024).pdfTechSoup
In this webinar you will learn how your organization can access TechSoup's wide variety of product discount and donation programs. From hardware to software, we'll give you a tour of the tools available to help your nonprofit with productivity, collaboration, financial management, donor tracking, security, and more.
Synthetic Fiber Construction in lab .pptxPavel ( NSTU)
Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
2. Asraful Islam Rayhan Rafiqul Islam
Shaharul Islam Assistant professor
Sadikur Rahman Dept. of pharmacy
Sohel Rana JUST
Arman Ahmed
Dept. of pharmacy
JUST
presented by, presented to,
3. CONTENT
Definition
Source
Chemistry
Structure activity relationship
Physical & chemical properties
Mechanism of action
Types of macrolide
Pharmacokinetics
Macrolide resistance
Spectrum of activity
Indication
Contraindication
Side effect
Market preparation
4. Macrolides
The macrolides are a group of antibiotics produced by
various strains of Streptomyces and having a macrolide
ring structure linked to one or more sugars. They act by
inhibiting protein synthesis, specifically by blocking the
50S ribosomal subunit. They are broad spectrum
antibiotics.
Examples: Erythromycin, Azithromycin, Clarithromycin,
Roxithromycin etc……………
5. SOURCE:
These Are Produced By Streptomyces species.
CHEMISTRY:
A macro cyclic lactone, usually having 12 to 17 atoms.
A ketone group.
One or two amino sugars linked to the nucleus.
A neutral sugar linked either to amino sugar or to
lactone ring.
The presence of the dimethyl amino moiety on the
sugar residue, which explains the basicity of these
compounds and consequently formation salts.
7. As macrolide are unstable in acidic pH, a no. of strategies have been
utilized to improve the acidic stability of erythromycin.
The addition of hydroxylamine
to the ketone to form oxime
e.g. roxithromycin
Alteration of c-6 hydroxyl
group: nucleophilic
functionality which
initiates erythromycin degradation.
The azalides (azithromycin)are
semi- synthetic 15 -membered
congeners in which a nitrogen atom
has been introduced to expand a
14-membered precursor-leads to an extended spectrum of action.
8. Physical & Chemical properties
Water insoluble molecules.
Occurs as crystalline powders.
Stable in aqueous solutions at or bellow
room temperature.
Unstable in acidic conditions and forms
internal cyclic ketal.
9. Macrolide is a protein synthesis inhibitor:
Macrolide bind to 50S ribosomal subunit
Inhibit polypeptide chain elongation &
protein synthesis inhibition
Result in inhibition of growth &
multiplication
12. Physical properties:
Yellow to white crystalline powder.
Soluble in alcohol, slightly soluble in water.
Stable at neutral pH.
Dosage forms:
Oral and topical dosage forms.
Enteric coted and delayed realese dosage forms.
Drug interactions:
Anticoagulants
Benzodiazepines
Antihistaminic drugs
13. It is used in,
Streptococcal pharyngitis
Tonsillitis
Respiratory infection
Diphtheria
Tetanus
Syphilis & gonorrhoea
Whooping cough
16. Advantages
Cannot undergo cyclic ketal formation, so doesn’t
cause cramp in GI
Higher blood concentrations.
More lipophyl.
Lower doses with less intervals.
Uses:
Atypical mycobacterial infection
Resistant leprosy
Toxoplasmosis
H.Pylori induced peptic ulcers
17.
18.
19. In the treatment of Urogenital infections caused by
N.gonorrhoeae and Chlamydia trachomatis.
For the treatment of respiratory tract infections.
Pregnant women infected with scrub typhus:
Azithromycin can suitable for doxycyclin.
20.
21. properties:
Semi-synthetic 14–membered ring macrolide
antibiotic in which the erythronolide lactone ring has
been altered to prevent inactivation in the milieu.
Uses:
Active against both gram (+) & gram (-).
Treatment of skin ,dental & genital infections.
Treatment of upper & lower respiratory tract
infections.
22. Absorption:
Erythromycin-variable
absorption ,food may decrease
the absorption.
Clarithromycin-acid stable
& well absorbed regardless
of presence of food.
Azithromycin-acid stable,
food decreases absorption of capsules.
23. Distribution:
Extensive tissue & cellular distribution.
Clarithromycin & azithromycin with extensive
penetration.
Minimal CSF penetration.
Metabolism:
Via liver
24. Elimination:
Clarithromycin is the only macrolide partially
eliminated by the kidney.
Hepatically eliminated:(All)
None of the macrolides are removed during
hemodialysis.
25.
26. Gram Positive Aerobes
Erythromycin & Clarithromycin
display the best activity…........
Clarithro>Erythro>Azithro
Example:
• Stayphyloccous aureus
• Streptococcus pneumoniae
• Corynebacterium sp.
Gram negative Aerobes
Newer macrolides such as-
Azithromycin has enhanced
activity.
Azithro>Clarithro>Erythro
Example:
• H. influenzae
• Neisseria sp.
• Bordetella pertusis.
33. An introduction to medicinal chemistry; Graham L.
Patrick
Essentials of MEDICINAL PHARMACOLOGY; KD
Tripathy.
Foyel’s Principle of MEDICINAL CHEMISTRY.
Lippincott’s Pharmacology.
Qimp index of medicinal products & problem.
Basic & clinical pharmacology; katzumg, masters &
Trevor.
