This document defines anthelmintics as agents used to destroy or eliminate parasitic worms from the gastrointestinal tract. It classifies anthelmintics and discusses several common drugs used as anthelmintics including mebendazole, albendazole, thiabendazole, oxaminiquine, praziquantel, piperazine citrate, diethylcarbamazine citrate, pyrantel pamoate, oxentel, niclosamide, and ivermectin. The document provides details on the chemical structure, mechanism of action, and uses of many of these anthelmintic drugs.
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.
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.
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
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
Protozoal infections and antiprotozoal drugs(therapy).Gagandeep Jaiswal
presentation comprising knowledge about various protozoal infections and therapy options available for the treatment of those infections. various different drugs used in the therapy with their proposed mechanism of action. Hope it will be useful for understanding the pharmacology of antiprotozoals.
Tetracyclines slide contains full information about uses, adverse effect, marketed preparation, precaution, route of drug administration, antimicrobial spectrum, mechanism of action, pharmacokineticks and pharmacodynamics of tetracyclines. This slide is very helpful for pharmacy and pharmacology student for the study about tetracyclines.
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.
Basic principles of chemotherapy/ AMAs covers definition, history of AMAs development, principles of AMAs, problems associated with AMAs, failure of therapy with examples.
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
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
Protozoal infections and antiprotozoal drugs(therapy).Gagandeep Jaiswal
presentation comprising knowledge about various protozoal infections and therapy options available for the treatment of those infections. various different drugs used in the therapy with their proposed mechanism of action. Hope it will be useful for understanding the pharmacology of antiprotozoals.
Tetracyclines slide contains full information about uses, adverse effect, marketed preparation, precaution, route of drug administration, antimicrobial spectrum, mechanism of action, pharmacokineticks and pharmacodynamics of tetracyclines. This slide is very helpful for pharmacy and pharmacology student for the study about tetracyclines.
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.
Basic principles of chemotherapy/ AMAs covers definition, history of AMAs development, principles of AMAs, problems associated with AMAs, failure of therapy with examples.
Medicinal chemistry- Antineoplastic Agents-ALKYLATING Agents
description regarding the Structure-Activity Relationship of alkylating agents, mechanism of action of alkylating agents and its uses
Medicinal Chemistry of Steroidal Harmons
Classification of Steroidal Harmons
Medicinal Uses
Biosynthesis of Steroidal Harmons
Mechanism of action of Steroidal Harmons
Natural and Synthetic derivatives of Steroidal Harmons and their Inhibitors
Introduction to types of Fungal Infections
Classification of Anti Fungal Agents
Chemistry of anti fungal agents
Azole Anti Fungal Agents
Mechanism of Action (MOA)
Structural Activity Relationship (SAR)
Prodrug is a pharmacological substance administered in an inactive form.
Once administered, the prodrug is metabolized in vivo into an active drug within the body through metabolic process, such as hydrolysis of an ester form of the drug.
Professional air quality monitoring systems provide immediate, on-site data for analysis, compliance, and decision-making.
Monitor common gases, weather parameters, particulates.
Nutraceutical market, scope and growth: Herbal drug technologyLokesh Patil
As consumer awareness of health and wellness rises, the nutraceutical market—which includes goods like functional meals, drinks, and dietary supplements that provide health advantages beyond basic nutrition—is growing significantly. As healthcare expenses rise, the population ages, and people want natural and preventative health solutions more and more, this industry is increasing quickly. Further driving market expansion are product formulation innovations and the use of cutting-edge technology for customized nutrition. With its worldwide reach, the nutraceutical industry is expected to keep growing and provide significant chances for research and investment in a number of categories, including vitamins, minerals, probiotics, and herbal supplements.
Cancer cell metabolism: special Reference to Lactate PathwayAADYARAJPANDEY1
Normal Cell Metabolism:
Cellular respiration describes the series of steps that cells use to break down sugar and other chemicals to get the energy we need to function.
Energy is stored in the bonds of glucose and when glucose is broken down, much of that energy is released.
Cell utilize energy in the form of ATP.
The first step of respiration is called glycolysis. In a series of steps, glycolysis breaks glucose into two smaller molecules - a chemical called pyruvate. A small amount of ATP is formed during this process.
Most healthy cells continue the breakdown in a second process, called the Kreb's cycle. The Kreb's cycle allows cells to “burn” the pyruvates made in glycolysis to get more ATP.
The last step in the breakdown of glucose is called oxidative phosphorylation (Ox-Phos).
It takes place in specialized cell structures called mitochondria. This process produces a large amount of ATP. Importantly, cells need oxygen to complete oxidative phosphorylation.
If a cell completes only glycolysis, only 2 molecules of ATP are made per glucose. However, if the cell completes the entire respiration process (glycolysis - Kreb's - oxidative phosphorylation), about 36 molecules of ATP are created, giving it much more energy to use.
IN CANCER CELL:
Unlike healthy cells that "burn" the entire molecule of sugar to capture a large amount of energy as ATP, cancer cells are wasteful.
Cancer cells only partially break down sugar molecules. They overuse the first step of respiration, glycolysis. They frequently do not complete the second step, oxidative phosphorylation.
This results in only 2 molecules of ATP per each glucose molecule instead of the 36 or so ATPs healthy cells gain. As a result, cancer cells need to use a lot more sugar molecules to get enough energy to survive.
Unlike healthy cells that "burn" the entire molecule of sugar to capture a large amount of energy as ATP, cancer cells are wasteful.
Cancer cells only partially break down sugar molecules. They overuse the first step of respiration, glycolysis. They frequently do not complete the second step, oxidative phosphorylation.
This results in only 2 molecules of ATP per each glucose molecule instead of the 36 or so ATPs healthy cells gain. As a result, cancer cells need to use a lot more sugar molecules to get enough energy to survive.
introduction to WARBERG PHENOMENA:
WARBURG EFFECT Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside.
Otto Heinrich Warburg (; 8 October 1883 – 1 August 1970) In 1931 was awarded the Nobel Prize in Physiology for his "discovery of the nature and mode of action of the respiratory enzyme.
WARNBURG EFFECT : cancer cells under aerobic (well-oxygenated) conditions to metabolize glucose to lactate (aerobic glycolysis) is known as the Warburg effect. Warburg made the observation that tumor slices consume glucose and secrete lactate at a higher rate than normal tissues.
This pdf is about the Schizophrenia.
For more details visit on YouTube; @SELF-EXPLANATORY;
https://www.youtube.com/channel/UCAiarMZDNhe1A3Rnpr_WkzA/videos
Thanks...!
The increased availability of biomedical data, particularly in the public domain, offers the opportunity to better understand human health and to develop effective therapeutics for a wide range of unmet medical needs. However, data scientists remain stymied by the fact that data remain hard to find and to productively reuse because data and their metadata i) are wholly inaccessible, ii) are in non-standard or incompatible representations, iii) do not conform to community standards, and iv) have unclear or highly restricted terms and conditions that preclude legitimate reuse. These limitations require a rethink on data can be made machine and AI-ready - the key motivation behind the FAIR Guiding Principles. Concurrently, while recent efforts have explored the use of deep learning to fuse disparate data into predictive models for a wide range of biomedical applications, these models often fail even when the correct answer is already known, and fail to explain individual predictions in terms that data scientists can appreciate. These limitations suggest that new methods to produce practical artificial intelligence are still needed.
In this talk, I will discuss our work in (1) building an integrative knowledge infrastructure to prepare FAIR and "AI-ready" data and services along with (2) neurosymbolic AI methods to improve the quality of predictions and to generate plausible explanations. Attention is given to standards, platforms, and methods to wrangle knowledge into simple, but effective semantic and latent representations, and to make these available into standards-compliant and discoverable interfaces that can be used in model building, validation, and explanation. Our work, and those of others in the field, creates a baseline for building trustworthy and easy to deploy AI models in biomedicine.
Bio
Dr. Michel Dumontier is the Distinguished Professor of Data Science at Maastricht University, founder and executive director of the Institute of Data Science, and co-founder of the FAIR (Findable, Accessible, Interoperable and Reusable) data principles. His research explores socio-technological approaches for responsible discovery science, which includes collaborative multi-modal knowledge graphs, privacy-preserving distributed data mining, and AI methods for drug discovery and personalized medicine. His work is supported through the Dutch National Research Agenda, the Netherlands Organisation for Scientific Research, Horizon Europe, the European Open Science Cloud, the US National Institutes of Health, and a Marie-Curie Innovative Training Network. He is the editor-in-chief for the journal Data Science and is internationally recognized for his contributions in bioinformatics, biomedical informatics, and semantic technologies including ontologies and linked data.
THE IMPORTANCE OF MARTIAN ATMOSPHERE SAMPLE RETURN.Sérgio Sacani
The return of a sample of near-surface atmosphere from Mars would facilitate answers to several first-order science questions surrounding the formation and evolution of the planet. One of the important aspects of terrestrial planet formation in general is the role that primary atmospheres played in influencing the chemistry and structure of the planets and their antecedents. Studies of the martian atmosphere can be used to investigate the role of a primary atmosphere in its history. Atmosphere samples would also inform our understanding of the near-surface chemistry of the planet, and ultimately the prospects for life. High-precision isotopic analyses of constituent gases are needed to address these questions, requiring that the analyses are made on returned samples rather than in situ.
2. DEFINITION
Are the agents which are used to
destroy (or) eliminate parasitic
worms (HELMINTH) from the GIT.
act by killing (or) paralysing the
worms.
So that such worms could be easily
expelled out of gut.
3. REPRODUCTION
These parasitic worms firmly hold the intestinal mucosa and
continue their reproduction by egg production.
They harm the host by depriving them of
Food
Causing blood loss
Injury to organs
Intestinal & lymphatic
obstruction
Secreting toxins
4. ■ Adult filariae live in the lymphatics,
connective tissue or mesentery of host and
produce live embryos or microfilariae,
which goes to blood stream.
■ They are ingested by mosquitoes or similar
insects, they develop to larvae in
secondary host and pass to mouth parts of
insect and
re-injected to humans
12. TYPES OF ANTHELMINTICS
■ Depending upon the action, anthelmintics can be categorised
into
■Vermifuges expel the worms
from the body
■Vermicides kill the worms in
the body
16. MEBENDAZOLE
■ Vermox
■ Methyl-5-benzoyl-2-benzimidazolyl carbamate.
■ MOA- It irreversibly blocks glucose uptake in susceptible
helminths, therby depleting glycogen stored in the parasite.
■ It does not affect glucose metabolism in the host.
N
H
N
NH COCH3
O
C
18. SYNTHESIS
C
SCH3
H2N NH
ClCOOCH3
S-methyl thio urea
methyl chloro
formate
C
SCH3
H2N NCOOCH3
NaOH
PH 8
Methyl-s-methyl
thio urea carbamate
STEP 1
STEP 2
O
C
Cl
4-Chloro benzo
phenone
HNO3
O
C
Cl
NO2
NH3
O
C
NH2
H2-Pd-C
NO2
O
C
NH2
NH2
C
SCH3
H2N NCOOCH3
O
C
N
H
N
NHCOOCH3
-NH3
-CH3SH
19. ALBENDAZOLE
■Eskazole, Zentel
■Methyl 5-(propylthio)-2-benzimidazole carbamate
■Widely employed throughout the world for the treatment of intestinal
nematode function.
■Is effective as a single dose treatment for
Ascariasis
Hookworm infections
Trichuriasis
N
H
N
NH COOCH3
S
21. MECHANISMOF ACTION
bind with β-tubulin and inhibit microtubule polymerization.
β-tubulin is the precursor of formation of microtubules.Thereby
arrest in cell division in nematodes.
■Biochemical Changes
■Inhibition of mitochondrial fumerate reductase
■Reduced glucose transport
■Uncoupling of oxidative phosphorylation
22. THIABENDAZOLE (cont)
■It has a broad spectrum anthelmintic activity.
■Used to treat
■Enterobiasis (thread worm)
■Ascariasis (round worm)
■Trichuriasis (whip worm)
■In addition to its use in human medicine, it is
widely employed in vertinary practice to control
helminths.
24. OXAMNIQUINE
■ Vansil
■ 1,2,3,4-tetrahydro-2-[isopropyl-amino) methyl]-7-nitro-6-
quinoline methanol.
■ It inhibits DNA, RNA & protein synthesis.
■ SAR- OH group is essential for activity.
■ For the treatment of intestinal schistosomiasis.
N
H
O2N
HOH2C
CH2NHCH
25. PRAZIQUANTEL
■ Biltricide
■ 2-(cyclohexyl carbonyl)-1,2,3,6,7,11b-hexahydro-4H-
pyrazino[2,1-a]isoquinolin-4-one.
■ It increases cell membrane permeability of susceptible worms,
resulting in loss of intracellular calcium and loss of extracellular
sodium.
N
N
C
O
26. ■ Massive contractions & ultimate
paralysis of the fluke musculature occurs.
■ The worms lose grip of intestinal mucosa
and are expelled.
■ USE- It has become the agent of choice
for the treatment of infections caused by
fluke infections
27. PIPERAZINE CITRATE
Artheriticine, Dispermin
MOA: It blocks the response of the ascaris muscle to acetyl
choline, causing the flaccid paralysis in the worm, which is
dislodged from the intestinal wall and expelled in the feces.
Highly effective againstAscaris lumbricoides & Enterobius
vermicularis.(Round worm & thread worm)
N
H
H
N
30. Mechanism Of Action
■Immobilizes microfilariae and alters their surface structure,displacing them from
tissues & making them susceptible to destruction by host defense mechanism
■ It has immunosuppressive effects
■Filariasis and ascariasis
34. Oxentel
Oxantel pamoate is an agonist of the acetylcholine receptors in the
muscle of nematodes and causes paralysis.
35. NICLOSAMIDE
■ Cestocide, Mansonil,Yomesan
■ 5-chloro-N-(2-chloro
-4 nitrophenyl)-2-hydroxy
benzamide
■ MOA:The drug inhibits anerobic phosphorylation ofADP
by the mitochondria of the parasite, and interfering with
anerobic generation of ATP by theTape worm.
■ So it inhibits seperation and blocking glucose absorption
by the intestinal nematode function.
OH
Cl
C
O
NH NO2
Cl
36. ■ SAR- For the activity, the OH group of benzoic acid moiety had
to be in 2 nd position.
■ Uses-Agent for choice for the treatment ofTaenia solium and
Taenia saginata.
■ A saline purge 1-2 hr after the ingestion of this drug is
recommended to remove the damaged scolex & worm
infections.
■ Quinacrine can aid for this purpose.
38. ■ Are a mixture of 22,23dihydro derivatives of avermectins B1a
&B1b prepared by catalytic reduction.
■ Are members of a family of structurually complex antibiotics
produced by a strain of Sterptomyces avermilitis.
■ The structures of avermectins were established by a
combination of spectroscopic and X-ray crystallographic
techniques to contain pentacyclic aglycone glycosidically linked
at 13 th position to a disaccharide that comprises two
oleandrose sugar residues.
■ MOA- It blocks interneuron transmission in nematodes by
stimulating the release of inhibitory neurotransmitter γ-amino
butyric acid-GABA.
■ Uses- widespread use in veterinary practice in the treatment of
Onchocerciasis caused by Oncocerca volvulus.
