medicinal chemistry of antiviral drugs with its chemical structures and how they chemically work
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
antiviral drugs medicinal chemistry by padala varaprasadVaraprasad Padala
medicinal chemistry of antiviral drugs by padala varaprasad
mainly includes structures, SAR , mechanism of action, uses and toxicity of antiviral drugs
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
antiviral drugs medicinal chemistry by padala varaprasadVaraprasad Padala
medicinal chemistry of antiviral drugs by padala varaprasad
mainly includes structures, SAR , mechanism of action, uses and toxicity of antiviral drugs
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
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watch video:https://www.youtube.com/watch?v=v3rI1lf2TZ8&t=403s
This slide describes the Important Synthesis of Antiviral Drugs
sulfonamides are the antimicrobial agents.It's act by folic acid synthesis inhibitors.It is PABA analogue competitive antagonist. first synthesised drug is prontosil.
In this slide contents history, mechanism of action, SAR, classification of drugs, some structure of important drugs, choice of drugs in different purpose, side effect, adverse effect.
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
Sulphonamides, MOA, SAR, History of development, Nomenclature of the Sulfonamides, Classification, Spectrum of Action of the Sulfonamides,Structure Activity Relationship, Reducing Toxicity, Cotrimoxazole
Anti viral drugs are a class of medication used specifically for treating viral infections.Viruses are obligate intracellular parasites, smallest of all self replicating organisms, able to pass through filter that retain the smallest bacteria.Virus conduct no metabolic process on their own.They invade the host cell which may be bacteria, animal or plant cell.
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watch video:https://www.youtube.com/watch?v=v3rI1lf2TZ8&t=403s
This slide describes the Important Synthesis of Antiviral Drugs
sulfonamides are the antimicrobial agents.It's act by folic acid synthesis inhibitors.It is PABA analogue competitive antagonist. first synthesised drug is prontosil.
In this slide contents history, mechanism of action, SAR, classification of drugs, some structure of important drugs, choice of drugs in different purpose, side effect, adverse effect.
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
Sulphonamides, MOA, SAR, History of development, Nomenclature of the Sulfonamides, Classification, Spectrum of Action of the Sulfonamides,Structure Activity Relationship, Reducing Toxicity, Cotrimoxazole
Anti viral drugs are a class of medication used specifically for treating viral infections.Viruses are obligate intracellular parasites, smallest of all self replicating organisms, able to pass through filter that retain the smallest bacteria.Virus conduct no metabolic process on their own.They invade the host cell which may be bacteria, animal or plant cell.
Antiviral drugs are a class of medications used to treat viral infections by inhibiting the replication or growth of viruses in the body. These drugs work by targeting specific components of a virus, such as the viral enzymes, proteins, or nucleic acids, and disrupting their ability to infect or replicate inside host cells. This can help reduce the severity of symptoms, prevent complications, and speed up recovery.
There are many types of antiviral drugs available, including:
1. Nucleoside or nucleotide analogues: These drugs mimic the structure of the nucleosides or nucleotides needed for viral replication, thereby interfering with virus replication.
2. Protease inhibitors: These drugs block the activity of viral proteases, which are enzymes that are required for the replication and assembly of some viruses.
3. Interferons: These drugs are naturally occurring proteins that help the immune system fight viral infections by boosting the body's antiviral response.
4. Neuraminidase inhibitors: These drugs block the activity of viral neuraminidase, an enzyme that is required for the release of virus particles from infected cells.
5. Fusion inhibitors: These drugs block the fusion of viral and host cell membranes, which is an essential step in viral entry and replication.
Antiviral drugs can be used to treat a variety of viral infections, including influenza, HIV/AIDS, hepatitis B and C, herpes, and Ebola. However, the effectiveness of these drugs can vary depending on the specific virus and the stage of infection. Antiviral drugs may also have side effects, and it is important to consult with a healthcare provider before taking them.
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.
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
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
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Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
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TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
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
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Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
2. • Viruses is a small infectious
agents that replicates only
inside the living cells of other
organisms.
• Viruses are lack both a cell wall
and cell membrane and they do
not carry out metabolic process
3. Viral particles consist of two to three parts :
1. Genetic material , either DNA or RNA
2. Protein coat (Capsid), which surrounds and
protects the genetic material
3. Envelope of lipid , lipid layer that surround the
protein coat when they are outside cell
• Viruses cannot reproduce on their
Own , they use host’s metabolic processes and
so few drugs are selective enough to prevent viral
replication
4. Viral attachment and
entry are blocked by:
• Enfuvirtide(HIV)
• Maraviroc(HIV)
• Docosanol(HSV)
• Palivizumab (RSV)
Uncoating are blocked by:
• Amantadine (influenza)
• Rimantadine(influenza)
Nucleic acid synthesis are
blocked by:
• Nucleoside reverse
transcriptase Inhibitors
NRTI (HIV,HBV)
• Non-Nucleoside reverse
transcriptase Inhibitors
NNRTI (HIV)
• Acyclovir (HSV)
• Foscarnet(CMV)
Protein processing are
blocked by:
• Protease inhibitors (HIV)
Viral release are blocked by:
• Neuraminidase
inhibitors(Influenzas)
5. Uncoating Inhibitors
• Amantadine and Rimantadine :
• They are hydrophobic amines
(weak organic bases) with clinical
against influenza A only.
• Their specificity stems from their
ability to bind to block the
proton channel formed by the
M2 matix protein.
• Can reduce severity of illness if
started within 48 hrs of onset of
symptoms .
6. Uncoating inhibitors
Amantadine :
Amantadine (1-aminoadamantane)
and its methyl derivative inhibit the
uncoating of the viral RNA within
the infected host cells thus
preventing its replication
10. •
The most common drugs that
prevent the virus from entering CD4
cells are:
-Maraviroc
-Enfuvirtide
-Docosanol
Entry Inhibitors:
11. Maraviroc:
-It is new class of antiretroviral agents that
targets a host protein, the chemokine
receptor CCR5, rather than a viral target.
-Binding to this cell-surface protein.
-block human immunodeficiency virus type
1 (HIV-1) attachment to the coreceptor and
prevents the virus from entering
CD4+ cells.
-Maraviroc is a substrate of cytochrome
P450 (CYP3A) and p-glycoprotein, and has
clinically significant interactions with other
drugs including efavirenz and rifampin.
14. Enfuvirtide
•New class of antiviral drug, fusion inhibitors, which interferate with penetration of
HIV-1 in the cells.
•Exhibits potent and selective inhibition of membrane of viral and cells.
•Showed significantly efficacy in the combination with other antiviral drugs in early
stadium of HIV infection and in patients with antiretroviral resistention
15. Protease inhibitors:
-the use of X-ray crystallography and molecular
modelling led to the structure-based design of a
series of inhibitors which act on the viral
enzyme HIV protease.
-They have a short-term benefit when they are
used alone, but resistance soon develops.
-When protease and reverse transcriptase
inhibitors are used together, the antiviral activity
is enhanced and viral resistance is slower to
develop.
16.
17. Saquinavir
-the first PI to reach the
market
- it has high molecular
weight and peptide-like
character
- oral bioavailability
19. Nucleic acid
Inhibitors
• These drugs usually act by
inhibiting the polymerases or
reverse transcriptase required for
nucleic acid synthesis. They are
usually analogues of the purine
and pyrimidine bases found in the
nucleic acids.
21. Acyclovir
• is the prototypic antiherpetic therapeutic agent. Herpes
simplex virus (HSV) types 1 and 2,varicella-zoster virus (VZV)
(i.e. chickenpox and shingles).
• Acyclovir has a nucleoside-like structure
• it lacks the complete sugar ring.
• In virally infected cells, it is phosphorylated to form a
triphosphate which is the active agent, and so acyclovir is a
prodrug
• Acyclovir triphosphate prevents DNA replication in two ways.
Firstly, it can bind to DNA polymerase and inhibit it.
Secondly, the drug acts as a chain terminator
22.
23. Valacyclovir
• The oral bioavailability of acyclovir is quite low (15– 30%).
• To overcome this, various prodrugs were developed to
increase water solubility. Valacyclovir is an l-valyl ester
prodrug absorbed from the gut far more effectively than
acyclovir.
24. Nucleoside reverse transcriptase inhibitors
(NRTI)
Zidovudine:
sugar 3′-hydroxyl
group
has been replaced by
an azido group
lamivudine and emtricitabine:
analogues of deoxycytidine
where the 3′ carbon has been
replaced by sulphur.
Didanosine:
nucleic acid base
present is inosine
base
25. • are analogs of native ribosides which all
lack a 3′-hydroxyl group.
• Once they enter cells, they are
phosphorylated to triphosphate analog
which is incorporated into the viral DNA
by Reverse Transcriptase . Because the
3′-hydroxyl group is not present, a 3′,5′-
phosphodiester bond between an
incoming nucleoside triphosphate and
the growing DNA chain cannot be
formed, and DNA chain elongation is
terminated
27. • are generally hydrophobic
molecules that bind to an
allosteric binding site
which is hydrophobic in
nature. Since the allosteric
binding site is separate
from the substrate binding
site, the NNRTIs are non-
competitive, reversible
inhibitors
28. Nevirapine
• Nevirapine has a rigid butterfly-like
conformation that makes it chiral. One
‘wing’ interacts through hydrophobic
and van der Waals interactions with
aromatic residues in the binding site,
while the other wing interacts with
aliphatic residues.
30. Release Inhibitors
• Drugs use to prevents the
Neuraminidase proteins on the
surface of IV removing sialic acid
from sialic aid-contanining
receptors .
• Viral budding and downstream
replication of IV are inhibited
when sialic acid remains on the
virion membrane and host cell.
• This segment will focus on the
synthesis of the anti-influenza
compound.
• available drugs : Zanamivir and
oseltamivir.
31.
32.
33. Oseltamivir
first orally active neuraminidase (NA) inhibitor.a prodrug
compound. Hydrolysis of the ester takes place in the body to
give the active carboxylic acid derivative of oseltamivir.
As a structural analogue of a key intermediate in sialic
acid/NA chemistry, oseltamivir serves as a competitive
inhibitor of viral NA by binding strongly to the active site of
NA. This interaction ultimately prevents the release of new
viral particles from the host cell.
Oseltamivir not a natural product but it is derived from
a natural product called shikimic acid.
34. Zanamivir
• Effective for both influenza A and B.
• Poor bioavailability and poor plasma portion
binding
• Use oral inhalation
4-guanidino-2,4-dideoxy-2,3-dehydro-N-
acetyl neuraminic aid
35. REFRENCES
• An Introduction to Medicinal Chemistry (5th
edition), Graham L. Patrick
• Fundamentals of Medicinal Chemistry,Gareth
Thomas
• Wilson and Gisvold’s Textbook of ORGANIC
MEDICINAL AND PHARMACEUTICAL CHEMISTRY
(12th edition)
• https://www.ncbi.nlm.nih.gov/pubmed/16134757
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC438
0148/