medicinal chemistry of antiviral drugs by padala varaprasad
mainly includes structures, SAR , mechanism of action, uses and toxicity of antiviral drugs
The document discusses the structure, life cycle, and classification of viruses as obligate intracellular parasites. It then summarizes the medicinal chemistry of various classes of anti-viral agents, including their synthesis and mechanisms of action. The main classes covered are adamantane derivatives like amantadine, purine nucleotides like acyclovir, pyrimidine nucleotides like trifluridine, and phosphorus derivatives like foscarnet. The anti-viral agents work by inhibiting viral DNA polymerase, incorporating into viral DNA, or substituting for thymidine in viral DNA synthesis.
Quinolones are synthetic antibacterial agents derived from nalidixic acid. Modern fluoroquinolones are classified into generations based on potency and spectrum of activity, with later generations having broader coverage. They work by inhibiting bacterial DNA gyrase and topoisomerase IV, preventing DNA replication. Common quinolones include norfloxacin for urinary tract infections, ciprofloxacin with activity against Pseudomonas, and sparfloxacin active against streptococci and anaerobes.
Urinary tract infections are mainly caused by bacteria like E. coli and Staphylococcus. Common symptoms include burning during urination and red or pink colored urine. Quinolones are a class of antibiotics that are highly effective against many infectious diseases, including those caused by bacteria in the urinary tract. Quinolones work by inhibiting the bacterial DNA gyrase enzyme, which is responsible for compacting DNA and allowing replication. Some examples of quinolones used to treat UTIs are ciprofloxacin, norfloxacin, and ofloxacin. Other classes of antibiotics that can be used to treat UTIs include nitrofurans, sulfa drugs, and methenamine.
This document discusses the synthesis, mechanisms, properties, and uses of several antifungal drugs: Metronidazole, Ketoconazole, Terconazole, and Miconazole. It provides details on the synthesis routes for each drug involving reactions of intermediates. The mechanisms of action involve inhibiting enzymes necessary for fungal cell wall synthesis or metabolism, which damages DNA and leads to cell death. The properties described include melting points, solubility, and physical forms. All four drugs are used as broad-spectrum antifungal agents to treat various fungal infections.
The document discusses prodrug design and its applications. Prodrugs are biologically inert derivatives of drug molecules that undergo conversion in vivo to release the active parent drug. The objectives of prodrug design are to improve pharmaceutical and pharmacokinetic properties like solubility, stability, absorption and bioavailability. Prodrugs can be classified based on the carrier group attached and site of bioactivation. Applications include masking taste/odor, reducing irritation, enhancing solubility, stability and bioavailability to improve drug delivery. In summary, prodrug design is a strategy to overcome undesirable drug properties and improve therapeutic effectiveness.
The document discusses various approaches used in drug design, including quantitative structure activity relationship (QSAR) analysis. QSAR uses physicochemical parameters like partition coefficient, electronic parameters, and steric parameters to develop mathematical models correlating a drug molecule's structure to its biological activity. The goal is to predict activity for new compounds and guide drug design. Parameters commonly used in QSAR include log P for hydrophobicity, Hammett constants for electronics, and Taft constants for sterics. Methods involve Hansch analysis, Free Wilson models, and other statistical techniques.
The document discusses the structure, life cycle, and classification of viruses as obligate intracellular parasites. It then summarizes the medicinal chemistry of various classes of anti-viral agents, including their synthesis and mechanisms of action. The main classes covered are adamantane derivatives like amantadine, purine nucleotides like acyclovir, pyrimidine nucleotides like trifluridine, and phosphorus derivatives like foscarnet. The anti-viral agents work by inhibiting viral DNA polymerase, incorporating into viral DNA, or substituting for thymidine in viral DNA synthesis.
Quinolones are synthetic antibacterial agents derived from nalidixic acid. Modern fluoroquinolones are classified into generations based on potency and spectrum of activity, with later generations having broader coverage. They work by inhibiting bacterial DNA gyrase and topoisomerase IV, preventing DNA replication. Common quinolones include norfloxacin for urinary tract infections, ciprofloxacin with activity against Pseudomonas, and sparfloxacin active against streptococci and anaerobes.
Urinary tract infections are mainly caused by bacteria like E. coli and Staphylococcus. Common symptoms include burning during urination and red or pink colored urine. Quinolones are a class of antibiotics that are highly effective against many infectious diseases, including those caused by bacteria in the urinary tract. Quinolones work by inhibiting the bacterial DNA gyrase enzyme, which is responsible for compacting DNA and allowing replication. Some examples of quinolones used to treat UTIs are ciprofloxacin, norfloxacin, and ofloxacin. Other classes of antibiotics that can be used to treat UTIs include nitrofurans, sulfa drugs, and methenamine.
This document discusses the synthesis, mechanisms, properties, and uses of several antifungal drugs: Metronidazole, Ketoconazole, Terconazole, and Miconazole. It provides details on the synthesis routes for each drug involving reactions of intermediates. The mechanisms of action involve inhibiting enzymes necessary for fungal cell wall synthesis or metabolism, which damages DNA and leads to cell death. The properties described include melting points, solubility, and physical forms. All four drugs are used as broad-spectrum antifungal agents to treat various fungal infections.
The document discusses prodrug design and its applications. Prodrugs are biologically inert derivatives of drug molecules that undergo conversion in vivo to release the active parent drug. The objectives of prodrug design are to improve pharmaceutical and pharmacokinetic properties like solubility, stability, absorption and bioavailability. Prodrugs can be classified based on the carrier group attached and site of bioactivation. Applications include masking taste/odor, reducing irritation, enhancing solubility, stability and bioavailability to improve drug delivery. In summary, prodrug design is a strategy to overcome undesirable drug properties and improve therapeutic effectiveness.
The document discusses various approaches used in drug design, including quantitative structure activity relationship (QSAR) analysis. QSAR uses physicochemical parameters like partition coefficient, electronic parameters, and steric parameters to develop mathematical models correlating a drug molecule's structure to its biological activity. The goal is to predict activity for new compounds and guide drug design. Parameters commonly used in QSAR include log P for hydrophobicity, Hammett constants for electronics, and Taft constants for sterics. Methods involve Hansch analysis, Free Wilson models, and other statistical techniques.
This document provides an overview of antiviral drugs, including their mechanisms of action, classifications, and examples. It discusses how antiviral drugs work by inhibiting viral replication and preventing the virus from multiplying, rather than destroying the pathogen. The main classes covered are nucleoside analogs, including purine and pyrimidine analogs like acyclovir and idoxuridine; non-nucleoside reverse transcriptase inhibitors like nevirapine; protease inhibitors used to treat HIV; and miscellaneous agents like foscarnet sodium. For each drug class, examples are given along with descriptions of their structures, mechanisms of action, therapeutic uses, and dosages.
Plasmodium parasites cause malaria in humans. The document discusses various antimalarial agents, including:
1. Chloroquine, a 4-aminoquinoline that inhibits heme polymerization in parasites and is effective against several Plasmodium species but resistance has developed.
2. Mefloquine, a quinoline-methanol with strong blood-stage activity against multidrug resistant P. falciparum.
3. Quinine, a cinchona alkaloid that remains effective against some resistant strains and has moderate activity against hepatic and transmission stages.
Combinatorial chemistry is a technique used to rapidly produce large libraries of potential drug molecules. It allows scientists to create and evaluate thousands of similar compounds in parallel. The key advantages are that it is faster and more economical than traditional drug discovery methods. Some challenges include ensuring diversity in the compound libraries and identifying the active components within mixture samples. Solid phase synthesis and parallel/mixed synthesis are common techniques used in combinatorial chemistry approaches.
-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.
This document discusses anti-protozoal drugs used to treat protozoan infections. It describes how protozoan infections are caused by organisms formerly classified as protozoa and are contracted through insect vectors or contact with infected substances. It then outlines several classes of pharmaceuticals used to treat protozoan diseases, including nitroimidazole derivatives like metronidazole, diloxanide, iodoquinol, pentamidine, atovaquone, and eflornithine. It provides details on the structures and mechanisms of action of these various antiprotozoal agents.
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.
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watch video:https://www.youtube.com/watch?v=v3rI1lf2TZ8&t=403s
This slide describes the Important Synthesis of Antiviral Drugs
This document discusses antiprotozoal agents used to treat various protozoal diseases. It begins by introducing common protozoal diseases like malaria, amoebiasis, and leishmaniasis that infect humans and animals in tropical countries. The document then classifies antiprotozoal drugs and describes several types and their mechanisms of action. Key drugs discussed include emetine, metronidazole, ornidazole, tinidazole, clioquinol, and iodoquinol. The mechanisms of these drugs involve inhibiting protein synthesis, binding to DNA or metal ions, or undergoing microbial reduction to produce reactive intermediates.
This document provides information about anti-viral drugs. It begins by defining viruses and their structure. It then discusses different classes of anti-viral drugs, including those that block viral attachment and entry, inhibit penetration, act as uncoating inhibitors, and are nucleic acid inhibitors that target polymerases or reverse transcriptase. Specific drugs are discussed for each class, along with their mechanisms of action, structures, and importance for treating various viral diseases like HIV, hepatitis, herpes, and influenza.
medicinal chemistry of Antiviral drugsFatenAlsadek
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
Antimalarial agents are chemotherapeutic agents used to prevent and treat malaria caused by protozoan parasites of the genus Plasmodium. There are four main species that cause human malaria: P. malariae, P. vivax, P. falciparum, and P. ovale. Common antimalarial classes include 4-aminoquinolines like chloroquine, quinoline-methanols like mefloquine, cinchona alkaloids like quinine, and diaminopyrimidines like pyrimethamine. These work by accumulating in the parasite and raising vesicular pH to interfere with hemoglobin degradation or through other mechanisms like oxidative damage. Artemisinins
This document discusses several antiviral drugs including acyclovir, ribavirin, and tromantadine hydrochloride. It outlines their mechanisms of action, classifications, structures, and therapeutic uses for treating various viruses. Acyclovir is a nucleoside analogue that acts by terminating viral DNA chain elongation. Ribavirin has broad activity against RNA and DNA viruses by inhibiting viral mRNA capping and GTP synthesis. Tromantadine inhibits viral penetration and uncoating to block herpes simplex virus replication.
Viruses are obligate intracellular parasites that invade host cells and hijack their machinery to replicate. Antiviral drugs work by inhibiting viral replication and development inside host cells. There are several classes of antiviral drugs including adamantane derivatives, purine nucleotides, and pyrimidine nucleotides. Acyclovir, a purine nucleotide, gets activated by viral thymidine kinase inside infected cells and competitively inhibits viral DNA polymerase or gets incorporated into viral DNA. Idoxuridine, a pyrimidine nucleotide, is phosphorylated and substitutes for thymidine during viral DNA synthesis, inhibiting the viral DNA polymerase enzyme. Antiviral drugs display specificity against certain viruses by exploiting differences between host and viral polymer
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
Sulfonamides are antibacterial drugs that work by interfering with bacterial synthesis of folic acid. They are structural analogues of para-aminobenzoic acid (PABA) that bind to and inhibit the enzyme dihydropteroate synthase. This document discusses the mechanism of action, classification, structure-activity relationships, and properties of sulfonamides. It provides examples of commonly used sulfonamides and details their structures, mechanisms, and applications in treatment. The document also addresses issues like ionization, crystalluria, and dissociation constants that are important for understanding sulfonamide properties and use.
HIV causes AIDS by infecting immune cells and weakening the immune system. It is transmitted through bodily fluids and can be prevented by safe sex practices and not sharing needles. The virus attaches to CD4 receptors and integrates its DNA into host cells. This leads to reduced CD4 counts and opportunistic infections defining AIDS. Treatment involves antiretrovirals that target different stages of the viral lifecycle to suppress the virus and ART to control the disease.
Antiviral drugs work by interfering with the viral life cycle in various ways such as inhibiting viral nucleic acid synthesis, regulation, or the virus's ability to bind to and enter cells. There are several classes of antiviral drugs that target specific viruses including anti-herpes drugs like acyclovir and famciclovir, anti-influenza drugs like amantadine and oseltamivir, anti-hepatitis drugs like ribavirin and adefovir, and anti-HIV drugs like zidovudine, lamivudine, and interferon alpha. Many antiviral drugs are prodrugs that require activation within cells by viral or cellular enzymes
This document provides an overview of antiviral drugs, including their mechanisms of action, classifications, and examples. It discusses how antiviral drugs work by inhibiting viral replication and preventing the virus from multiplying, rather than destroying the pathogen. The main classes covered are nucleoside analogs, including purine and pyrimidine analogs like acyclovir and idoxuridine; non-nucleoside reverse transcriptase inhibitors like nevirapine; protease inhibitors used to treat HIV; and miscellaneous agents like foscarnet sodium. For each drug class, examples are given along with descriptions of their structures, mechanisms of action, therapeutic uses, and dosages.
Plasmodium parasites cause malaria in humans. The document discusses various antimalarial agents, including:
1. Chloroquine, a 4-aminoquinoline that inhibits heme polymerization in parasites and is effective against several Plasmodium species but resistance has developed.
2. Mefloquine, a quinoline-methanol with strong blood-stage activity against multidrug resistant P. falciparum.
3. Quinine, a cinchona alkaloid that remains effective against some resistant strains and has moderate activity against hepatic and transmission stages.
Combinatorial chemistry is a technique used to rapidly produce large libraries of potential drug molecules. It allows scientists to create and evaluate thousands of similar compounds in parallel. The key advantages are that it is faster and more economical than traditional drug discovery methods. Some challenges include ensuring diversity in the compound libraries and identifying the active components within mixture samples. Solid phase synthesis and parallel/mixed synthesis are common techniques used in combinatorial chemistry approaches.
-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.
This document discusses anti-protozoal drugs used to treat protozoan infections. It describes how protozoan infections are caused by organisms formerly classified as protozoa and are contracted through insect vectors or contact with infected substances. It then outlines several classes of pharmaceuticals used to treat protozoan diseases, including nitroimidazole derivatives like metronidazole, diloxanide, iodoquinol, pentamidine, atovaquone, and eflornithine. It provides details on the structures and mechanisms of action of these various antiprotozoal agents.
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.
subscribe the channel :Work&Life Hobbies
watch video:https://www.youtube.com/watch?v=v3rI1lf2TZ8&t=403s
This slide describes the Important Synthesis of Antiviral Drugs
This document discusses antiprotozoal agents used to treat various protozoal diseases. It begins by introducing common protozoal diseases like malaria, amoebiasis, and leishmaniasis that infect humans and animals in tropical countries. The document then classifies antiprotozoal drugs and describes several types and their mechanisms of action. Key drugs discussed include emetine, metronidazole, ornidazole, tinidazole, clioquinol, and iodoquinol. The mechanisms of these drugs involve inhibiting protein synthesis, binding to DNA or metal ions, or undergoing microbial reduction to produce reactive intermediates.
This document provides information about anti-viral drugs. It begins by defining viruses and their structure. It then discusses different classes of anti-viral drugs, including those that block viral attachment and entry, inhibit penetration, act as uncoating inhibitors, and are nucleic acid inhibitors that target polymerases or reverse transcriptase. Specific drugs are discussed for each class, along with their mechanisms of action, structures, and importance for treating various viral diseases like HIV, hepatitis, herpes, and influenza.
medicinal chemistry of Antiviral drugsFatenAlsadek
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
Antimalarial agents are chemotherapeutic agents used to prevent and treat malaria caused by protozoan parasites of the genus Plasmodium. There are four main species that cause human malaria: P. malariae, P. vivax, P. falciparum, and P. ovale. Common antimalarial classes include 4-aminoquinolines like chloroquine, quinoline-methanols like mefloquine, cinchona alkaloids like quinine, and diaminopyrimidines like pyrimethamine. These work by accumulating in the parasite and raising vesicular pH to interfere with hemoglobin degradation or through other mechanisms like oxidative damage. Artemisinins
This document discusses several antiviral drugs including acyclovir, ribavirin, and tromantadine hydrochloride. It outlines their mechanisms of action, classifications, structures, and therapeutic uses for treating various viruses. Acyclovir is a nucleoside analogue that acts by terminating viral DNA chain elongation. Ribavirin has broad activity against RNA and DNA viruses by inhibiting viral mRNA capping and GTP synthesis. Tromantadine inhibits viral penetration and uncoating to block herpes simplex virus replication.
Viruses are obligate intracellular parasites that invade host cells and hijack their machinery to replicate. Antiviral drugs work by inhibiting viral replication and development inside host cells. There are several classes of antiviral drugs including adamantane derivatives, purine nucleotides, and pyrimidine nucleotides. Acyclovir, a purine nucleotide, gets activated by viral thymidine kinase inside infected cells and competitively inhibits viral DNA polymerase or gets incorporated into viral DNA. Idoxuridine, a pyrimidine nucleotide, is phosphorylated and substitutes for thymidine during viral DNA synthesis, inhibiting the viral DNA polymerase enzyme. Antiviral drugs display specificity against certain viruses by exploiting differences between host and viral polymer
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
Sulfonamides are antibacterial drugs that work by interfering with bacterial synthesis of folic acid. They are structural analogues of para-aminobenzoic acid (PABA) that bind to and inhibit the enzyme dihydropteroate synthase. This document discusses the mechanism of action, classification, structure-activity relationships, and properties of sulfonamides. It provides examples of commonly used sulfonamides and details their structures, mechanisms, and applications in treatment. The document also addresses issues like ionization, crystalluria, and dissociation constants that are important for understanding sulfonamide properties and use.
HIV causes AIDS by infecting immune cells and weakening the immune system. It is transmitted through bodily fluids and can be prevented by safe sex practices and not sharing needles. The virus attaches to CD4 receptors and integrates its DNA into host cells. This leads to reduced CD4 counts and opportunistic infections defining AIDS. Treatment involves antiretrovirals that target different stages of the viral lifecycle to suppress the virus and ART to control the disease.
Antiviral drugs work by interfering with the viral life cycle in various ways such as inhibiting viral nucleic acid synthesis, regulation, or the virus's ability to bind to and enter cells. There are several classes of antiviral drugs that target specific viruses including anti-herpes drugs like acyclovir and famciclovir, anti-influenza drugs like amantadine and oseltamivir, anti-hepatitis drugs like ribavirin and adefovir, and anti-HIV drugs like zidovudine, lamivudine, and interferon alpha. Many antiviral drugs are prodrugs that require activation within cells by viral or cellular enzymes
HIV causes AIDS by infecting and destroying helper T cells of the immune system. It is transmitted through bodily fluids and can be prevented by safe sex practices and not sharing drug needles. While there is no cure for AIDS, treatment aims to suppress HIV replication with antiretroviral drugs and manage opportunistic infections. Highly active antiretroviral therapy (HAART) uses a combination of different classes of antiretroviral drugs including nucleoside/nucleotide reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, CCR5 receptor antagonists, and integrase inhibitors. Long term adherence to HAART can effectively suppress HIV and prolong the lives of
This document provides information on antiviral and antiretroviral drugs. It begins by describing viruses and their replication processes. It then discusses several important viruses and the diseases they cause. The document outlines the mechanisms of replication for DNA, RNA, and retroviruses. It proceeds to classify antiviral drugs according to their therapeutic uses and mechanisms of action. Several specific antiviral and antiretroviral drugs are described in detail, including their mechanisms of action, pharmacokinetics, and side effects. The human immunodeficiency virus (HIV) and acquired immunodeficiency syndrome (AIDS) are also discussed.
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.
anti virals -medication used against viral actionTeena42750
This document discusses antiviral drugs and classifies them based on their mechanism of action and target viruses. It describes several classes of antiviral drugs including anti-herpes drugs like acyclovir and famciclovir, anti-influenza drugs like oseltamivir and zanamivir, and various classes of antiretroviral drugs used to treat HIV like nucleoside reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, protease inhibitors, and entry inhibitors. Each drug is discussed in terms of its mechanism of action, target virus, uses, and common side effects.
Etiology, pathophysiology, Pharmacotherapy of AIDS .pptxdrsriram2001
Definition of AIDS:
Acquired Immunodeficiency Syndrome (AIDS) is a late stage of HIV (Human Immunodeficiency Virus) infection. It is characterized by a severe depletion of the immune system, making the individual susceptible to opportunistic infections and certain cancers.
2. Etiology (HIV):
HIV Structure:
HIV is a retrovirus that primarily targets CD4+ T cells, a crucial component of the immune system.
The virus has two main types: HIV-1 and HIV-2, with HIV-1 being the most common and virulent worldwide.
3. Transmission:
Modes of Transmission:
HIV is primarily transmitted through unprotected sexual intercourse with an infected person.
It can also be transmitted through sharing of contaminated needles, from an infected mother to her child during childbirth or breastfeeding, and through blood transfusions with infected blood (though this is rare now due to blood screening).
4. Clinical Stages:
Acute HIV Infection:
Occurs within the first few weeks after exposure.
Presents with flu-like symptoms such as fever, fatigue, and swollen lymph nodes.
Chronic HIV Infection (Asymptomatic Stage):
Can last for several years with few or no symptoms.
The virus is actively replicating, and the immune system is gradually compromised.
Symptomatic HIV Infection (Symptomatic Stage):
As the immune system weakens, symptoms such as persistent fever, weight loss, and diarrhea may occur.
AIDS:
Diagnosed when the immune system is severely compromised, typically when the CD4+ T cell count falls below a critical threshold.
Opportunistic infections (e.g., Pneumocystis jirovecii pneumonia) and certain cancers (e.g., Kaposi's sarcoma) become more common.
5. Preventive Measures:
Condom Use:
Consistent and correct use of condoms during sexual intercourse helps prevent the sexual transmission of HIV.
Pre-Exposure Prophylaxis (PrEP):
Antiretroviral medications, when taken consistently by HIV-negative individuals at high risk, can prevent HIV infection.
Post-Exposure Prophylaxis (PEP):
Emergency treatment with antiretroviral drugs within 72 hours of potential exposure to HIV to prevent infection.
Needle Exchange Programs:
Reducing the sharing of needles among injecting drug users helps prevent the transmission of HIV.
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.
This document discusses antiviral agents for nonretrovirals. It begins by outlining the key learning objectives which are to describe viral infections, classification of antiviral agents, their mechanisms of action and resistance. It then classifies antiviral agents into non-retroviral and antiretroviral categories. Under non-retroviral agents, it describes treatments for influenza, herpes and hepatitis viruses. It provides details on specific drugs for each virus type, including their mechanisms of action, resistance and pharmacokinetics.
Herpes viruses are associated with diseases like cold sores and genital infections. There are several drugs that are effective against these viruses during acute infection, including acyclovir, cidofovir, foscarnet, ganciclovir, penciclovir/famciclovir, and trifluridine. These drugs work by incorporating into viral DNA or inhibiting viral polymerases. Highly active antiretroviral therapy (HAART) uses combinations of drugs from five classes to suppress HIV replication, including nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors, entry inhibitors, and integra
This document discusses antiviral drugs and summarizes their mechanisms and classifications. It describes how viruses work at a cellular level and replicates inside host cells. It then classifies antiviral drugs based on their mechanism of action, including how they target different stages of the viral life cycle like entry, replication, assembly and release. Specific drugs are explained like amantadine, which targets influenza viruses, and nucleoside analogues including acyclovir which act as chain terminators during viral DNA synthesis. Interferons are also summarized as potent natural antiviral proteins produced by infected cells.
This document provides information on antiviral drugs and their classification and mechanisms of action. It discusses different types of antiviral drugs used to treat HIV/AIDS including nucleoside reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, protease inhibitors, entry inhibitors, and integrase inhibitors. It also discusses antiviral drugs for other viruses like viral DNA polymerase inhibitors, neuraminidase inhibitors, and immunomodulators. Specific drugs are discussed in detail including their mechanisms of action, pharmacokinetics, clinical uses, and adverse effects.
Basic concept of virus for nursing and vaccine preventable viruses [Autosav...OlisaEnebeli1
This document provides an overview of virology and vaccine preventable viral diseases for nursing students. It defines viruses and their structure, classification, life cycle, and pathogenesis. Common vaccine preventable viral diseases that are discussed include measles, mumps, rotavirus, hepatitis A, hepatitis B, human papillomavirus, and more. The goals are for students to understand viruses, how they cause disease, methods of diagnosis and prevention including vaccines.
This document summarizes various anti-viral agents, including nucleoside analogs that inhibit viral DNA polymerase and reverse transcriptase. It discusses idoxuridine, trifluridine, acyclovir and other nucleoside analogs used to treat herpes viruses. It also covers reverse transcriptase inhibitors like zidovudine and didanosine used to treat HIV. Newer agents for HIV include protease inhibitors, entry inhibitors, integrase inhibitors and combination antiretroviral therapy, which is most effective at preventing drug resistance.
Antiviral Drugs – A Brief (Classification & Mechanism of Actions)Parth Thosani
This presentation gives you an overview of antiviral agents (both retro and non-retro viruses), focusing on the sites of actions, classification and class-wise mechanism of actions.
This document discusses antiviral drugs and their mechanisms of action. It describes several classes of antiviral drugs that target different stages of the viral lifecycle, including nucleoside analog reverse transcriptase inhibitors (NRTIs), protease inhibitors, and DNA polymerase inhibitors. Specific drugs mentioned include acyclovir, ganciclovir, didanosine, zidovudine, lamivudine, saquinavir, indinavir, and ritonavir. It provides details on how these drugs work, such as by incorporating into viral DNA/inhibiting viral enzymes or being phosphorylated into active metabolites that inhibit viral replication. The document also discusses treatment of various viral infections including HIV, hepatitis
Similar to antiviral drugs medicinal chemistry by padala varaprasad (20)
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This document provides guidelines for retrosynthetic analysis, breaking down molecules into simpler synthetic precursors through logical disconnections. It discusses key retrosynthetic principles and transformations, highlighting common functional group interconversions and synthetically useful reactions that can be exploited in a retrosynthetic sense. The document serves as a guide for envisioning multi-step synthesis routes by systematically deconstructing target molecules.
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9
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antiviral drugs medicinal chemistry by padala varaprasad
1. UNIVERSITY COLLEGE OF PHARMACEUTIALSCIENCES
K.U. CAMPUS
ANTIVIRAL DRUGS
Presented by
P.VARAPRASAD
HT.No.2004P-1026
M. Pharmacy, I semester,
Department Of Pharmaceutical Chemistry
University College Of Pharmaceutical Sciences
3. INTRODUCTION TO VIRUSES
• Viruses are obligate intracellular parasites.
• Virus can be defined as sub microscopic entity consisting of a single
nucleic acid surrounded by a protein coat and capable of replication only
within the living cells.
• Viruses are much smaller than prokaryotes, ranging in size from about 20–
300 nanometers.
• The infective, extracellular (outside the cell) form of a virus is called the
virion.
• Viruses that infect only bacteria are called bacteriophages and those that
infect fungi are termed mycophages . There are even some viruses called
virophages that infect other viruses.
• The origins of viruses are unclear: some may have evolved from plasmids
while others may have evolved from bacteria.
• Over 5,000 species of viruses have been discovered.
1
4. STRUCTURE OF VIRUS
Capsid - The capsid is the protein shell that encloses
the nucleic acid; with its enclosed nucleic acid, it is
called the nucleocapsid. This shell is composed of
protein organized in subunits known as capsomers.
Envelope - Many types of virus have a glycoprotein
envelope surrounding the nucleocapsid. The envelope
is composed of two lipid layers interspersed with
protein molecules (lipoprotein bilayer) and may contain
material from the membrane of a host cell as well as
that of viral origin.
Nucleic Acid - Just as in cells, the nucleic acid of each
virus encodes the genetic information for the synthesis
of all proteins. While the double-stranded DNA is
responsible for this in prokaryotic and eukaryotic cells,
only a few groups of viruses use DNA. Most viruses
maintain all their genetic information with the single-
stranded RNA.
Fig1.Structure of virus
Fig2. 2
5. TYPES OF VIRUSES
DNA-viruses: Contain mostly double-stranded DNA, a small number single-stranded DNA.DNA
viruses enter the cell nucleus and direct the generation of new viruses. poxviruses, herpes,
adenoviruses papilloma viruses.
RNA-viruses: Contain largely single-stranded RNA (ssRNA).RNA viruses do not enter the cell nucleus
(except the influenza virus).RNA retroviruses uses the viral reverse transcriptase to make a DNA copy
of the viral RNA, which is then integrated into the host genome.
influenza, measles, mumps,meningitis, poliomyelitis, retroviruses (AIDS), arenaviruses.
3
6. THE VIRAL LIFE CYCLE
1. Attachment. The virus recognizes and
binds to a host cell via a receptor
molecule on the cell surface.
2. Entry. The virus or its genetic
material enters the cell.
3. Genome replication and gene
expression. The viral genome is
copied and its genes are expressed to
make viral proteins.
4. Assembly. New viral particles are
assembled from the genome copies
and viral proteins.
5. Release. Completed viral particles exit
the cell and can infect other cells.
Fig4..
4
11. ANTIVIRAL DRUGS
• Antiviral drugs are a class of medication used for treating
viral infections
• Antiviral drugs do not destroy their target pathogen instead
they inhibit their development.
• In 1963, idoxuridine became the first antiviral compound to
be licensed by the US Food and Drug Administration (FDA)
for the topical treatment of herpes simplex virus (HSV)
keratitis.
• Currently, antiviral therapy is available only for a limited
number of infections.
• Most of the antiviral drugs currently available are used to treat
infections caused by HIV, herpes viruses, hepatitis B and C
viruses, and influenza A and B viruses.
9
15. Acyclovir
Mechanism of action
It is sufficiently similar to the “normal”
nucleosides, so that it can serve as substrate for
the viral DNA polymerases. Since the sugar lacks
the 3’ hydroxyl group it act as chain terminators
13
16. • Acyclovir is prodrug, that can only be converted into the phosphorylated form
by the viral thymidine kinase and hence do not interfere with DNA synthesis
in non-infected cells:
Clinical application
Acyclovir has potent activity against several DNA viruses including HSV-1, the
common cause of labial herpes (cold sore), and HSV-2, the common cause of genital
herpes. Varicella-zoster virus and some isolates of EBV are affected to a lesser extent by
acyclovir .
14
19. Zidovudine
Mechanism of action
• Intracellularly, zidovudine is phosphorylated to its active 5-triphosphate metabolite,
zidovudine triphosphate (AZT-TP). It acts by competitive inhibition of HIV-1 reverse
transcriptase (RT; the enzyme that HIV uses to make a DNA copy of its RNA)
Deoxythymidine
Zidovudine is a deoxythymidine analog. It is the
first licensed antiretroviral agent. It is the first drug
approved for treatment of HIV
• The RT uses zidovudine
triphosphate instead of thymidine
triphosphate for making DNA, and it
is the zidovudine triphosphate that
interferes with the RT
•Zidovudine can also be incorporated
into the growing viral DNA chain to
cause termination
17
20. Zidovudine
Clinical application
• Zidovudine is used in AIDS and AIDS-related complex (ARC) to control
opportunistic infections by raising absolute CD4 lymphocyte counts.
Side effects
• The most common adverse effect of zidovudine is myelosuppression,
resulting in anemia or neutropenia.
• GI intolerance, headaches, and insomnia may occur but tend to resolve during
therapy.
18
21. Stavudine
• Stavudine is a pyrimidine nucleoside analogue that has significant activity
against HIV-1 after intracellular conversion of the drug to a D4T-triphosphate.
• The first mesylation of thymidine (I) to give dimesylate (II), which is treated with
sodium hydroxide in ethanol to yield oxetane (III). Finally, (III) is converted to
stavudine by means of potassium tert-butoxide in DMSO.
19
stavudine
synthesis
23. Nevirapine
Clinical application
• Nevirapine and its analogues exhibit antiretroviral effect against azothymidine-
resistant HIV strains
Side effects
• nausea
• loss of appetite
• upper stomach pain
• tiredness
• fever
• unexplained muscle pain
• dark urine
• jaundice
Mechanism of action
Nevirapine is a dipyridodiazepinone derivative that binds
directly to RT. Thus, it blocks RT activities by causing a
disruption of the enzyme's catalytic site. The activity of
nevirapine does not compete with template or nucleoside
triphosphate.
21
24. Antiviral agents interfering with
cellular penetration and early replication
Generic Name Trade Name Spectrum of
Activity
Dosage Form
Amantadine Symmetrel Influenza A Capsule (100mg),
Syrup(50 mg/5mL)
Rimantadine Flumadine Influenza A Capsule (100mg)
Oseltamivir Tamiflu Influenza A and B Capsule (75mg)
Zanamivir Relenza Influenza A and B Inhaled powder
(5mg)
Table 7. Antiviral Agents Interfering with Cellular Penetration and Early Replication
22
26. ANTIVIRAL AGENTS INTERFERING WITH
CELLULAR PENETRATION AND EARLY REPLICATION
24
Fig7.Antiviral agents interfering with cellular penetration and early replication , acting on influenza
27. Amantadine
• Adamantane derivatives block the migration of protons into the interior of the virions
within endosomes, thereby preventing the pH shift required for uncoating. They act
by blocking the M2 (matrix 2) channel.
structure activity relationship
Amantadine is a adamantane amine
• α –amino derivative of adamantane is amantadine
• N-Alkyl and N,N-dialkyl derivatives of adamantadine exhibit antiviral
activity similar to that of adamantadine HCl.
• Except glycyl derivatives, N–acyl derivatives shows decreased antiviral action
• Replacement of the amino group with OH, SH, CN, or halogen produced inactive
compounds.
Mechanism of action
It inhibits penetration of RNA viral partcles into the
host cell . It also inhibits the early stages of viral
replication by blocking the uncoating of the viral
genome and the transfer of nucleic acid into the host
cell.
25
28. Amantadine
Clinical application
• Amantadine is clinically effective in preventing and treating all type A
strains of influenza, particularly type A2 strains of Asian influenza
virus, and to a lesser extent , German measles (rubella) or atoga virus. It is
also used for parkinsonism
Side effects
• Generally, at therapeutic levels may cause severe CNS symptoms, such as
nervousness, confusion, headache, drowsiness, insomnia, depression,
and hallucinations. The GI side effects include nausea, diarrhea,
constipation, and anorexia. Convulsions and coma occur with high doses
and in patients with cerebral arteriosclerosis and convulsive disorders.
26
29. Neuraminidase Inhibitors(influenza)
• The influenza virus binds to the target cell via interaction of its surface
glycoprotein, haemagglutinin, with the host-cell surface receptor, that
contains sialic acid. Neuraminidase catalytically cleaves glycosidic bonds
between terminal sialic acid residues and adjacent sugars on hemagglutinin.
Allowing the virus to leave the cell once the virus has replicated
• Inhibiting the viral Neuraminidase prevents the virus from leaving the cell
and infecting others.
27
Fig8. Mechanism of Neuraminidase Inhibitors(influenza)
30. Oseltamivir (Tamiflu)
Clinical application
• Oseltamivir is used to treat symptoms caused by the flu virus (influenza). It helps
make the symptoms (such as stuffy nose, cough, sore throat, fever/chills, aches,
tiredness) less severe and shortens the recovery time by 1-2 days.
Side effects
• Nausea
• Vomiting
• Diarrhea
• Dizziness
• Headache
• Nosebleed
• Eye redness
• Sleep problems
• Cough
Mechanism of Action
Oseltamivir inhibits the neuraminidase enzyme,
which is expressed on the viral surface. The enzyme
promotes release of virus from infected cells
28
Fig9. Mechanism of Oseltamivir
(Oseltamivir)
31. PROTEASE INHIBITORS
• Protease cleave the viral polyproteins into individual functional HIV
proteins and enzymes. The various structural components then assemble to
produce a mature HIV virions which is capable of infecting another cell
• Drugs that inhibit HIV protease are designed as transition-state mimetics
that align at the activesite of HIV-1 protease
29
Fig10.Protease inhibitors
32. PROTEASE INHIBITORS
Generic Name Common Name Trade Name Dosage Form
Ritonavir RTV Norvir Capsule (200mg)
Atazanavir ATZ Reyataz Capsule(150and200mg)
Indinavir IDV Crixivan Capsule(200and400mg)
Nelfinavir NFV Viracept Tablet (250 mg),
powder(50mg/g)
Saquinavir Invirase
Fortovase
Capsule (200mg)
Capsule (200mg)
Amprenavir APV Agenerase Capsule(50and150mg)
solution (15mg/mL)
Lopinavir LPV Kaletra Capsule(133.3/33.3mg),
solution (80/20mg/mL)
Table8.Protease Inhibitors
30
34. Saquinavir
Mechanism of action
• It is specifically designed to inhibit HIV protease, thus preventing post translat ional
format ion of viral proteins.
• It contains a hydroxyethylamine moiety rather than the Phe-Pro scissile bond present
in the normal substrate for HIV protease.
Clinical application
• Saquinavir is used in the treatment of advanced HIV infection in selected patients.
Side effects
• GI disturbances,
• Headache
• Rhinitis
• Diarrhea.
Saquinavir was the first PI approved by the U.S.
FDA in December 1995. It is a carboxamide
derivative.
32
35. Fusion inhibitor:Enfuvirtide
enfuvirtide is the first compound of this family to be approved for clinical use.
Enfuvirtide is an oligo peptide consisting of 36 amino acids.
33
36. Enfuvirtide
Mechanism of action
• It is a synthetic peptide that mimics an HR2 fragment of gp41, blocking the
formation of a six-helix bundle structure that is critical in the fusion of the
HIV-1 virion to a CD4-positive T lymphocyte. Specifically, it binds to the
tryptophan-rich region of the gp41 protein.
Clinical application
• Enfuvirtide is used in combination with other antiretrovirals and works
against a variety of HIV-1 variants, but it is not active against HIV-2.
Side effects
• Injection site reactions, including itching, swelling, redness, pain or
discomfort, rash, bruising, hardened skin
• Nerve pain (neuralgia) or numbness, burning, or prickling feeling of your
skin (paresthesia) that lasts up to 6 months.
34
37. CCR5 receptor inhibitor: Maraviroc
Mechanism of action
• Maraviroc selectively binds to the human
chemokine receptor CCR5, which is
present on the cell membrane.
• This binding prevents the interaction of
HIV-1 gp 120 with CCR5-tropic HIV-1
and thereby inhibits the virus from
entering the cell.
35
Fig11.Mechanism of action of maraviroc
38. Maraviroc
Clinical application
• Maraviroc is used with other medications to treat CCR5-tropic HIV type 1.
Side effects
• Maraviroc is generally well tolerated with the incidence of diarrhea, nausea,
headache, and fatigue similar to or less than those of placebo.
• The most common adverse reactions in clinical studies are upper respiratory tract
infection, cough, pyrexia, rash and dizziness.
36
39. Integrase inhibitor:
• Integrase is a viral enzyme that catalyses both 3’ processing of viral DNA
in the cytoplasm, and insertion of the viral DNA into chromosomal DNA
in the nucleus
• Integrase inhibitors (INIs) are a class of antiretroviral drugs designed to
block the action of integrase.
• Since integration is a vital step in retroviral replication, blocking it can halt
further spread of the virus.
nucleus
cell
37
Fig12.mechanism of action of Integrase inhibitor
40. Raltegravir
Mechanism of action
• Raltegravir inhibits the activity of HIV-1 integrase, which impedes the insertion of
HIV-1 DNA into the host cell genome. It inhibits integration at an IC50 of ~10 nM
and the results are consistent with inhibition of the third step of the integration
process (i.e. strand transfer).
Clinical application
• Raltegravir is used along with other medications to treat HIV infection.
Side effects
• pale skin
• stomach pain,
• headache,
• tired feeling,
• dizziness,
• sleep problems (insomnia)
38
41. Interferons
• Interferons belong to the class of cytokines involved in cell-cell signaling,
particularly relating to the early detection of microbialinvasion
• IFNα and IFNβ are produced by most human cells in response to a viral
infection
• Production of interferons is mediated through activation of toll-like receptors
• Its production is transient and requires stimulation by viruses, microbial products
and other inducers
• Their action is mediated through the JAK/STAT and other signaling pathways
• They induce expression of 2,5-oligoadenylate synthase, which in turn produces
oligoadenylate that activates ribonuclease L, resulting in the degradation of
single-stranded RNA, and triggers cellular apoptosis
• IFNs are used to treat hepatitis B and C viral infections
39
42. Conclusion
• Viral infections are a major global health threat. Over the last 50 years, significant
efforts have been devoted to the development of antiviral drugs and great success has
been achieved for some viruses. However, other virus infections, such as epidemic
influenza, still spread globally and new threats continue to arise from emerging and re-
emerging viruses and drug-resistant viruses.
• Even with the most familiar virus targets, there is a continuing need to develop new
drugs or ingenious combinations of drugs that result in greater specificity ( less
toxicity) and increased drug-resistance barriers.
• In the period from 1996 to 2019 we almost halved the number of new HIV infections
and for the millions of people who still live with the virus, ARV treatment enables most
to lead long and healthy lives . A world without HIV is no longer inconceivable.
40
43. References
1. John B. Carter and Venetia A. Saunders. Virology Principles and applications.2013,2,31-48.
2. Arti Kapil, Paniker, Ananthanarayan. Textbook of Microbiology.2013,9,427-570
3. KD Tripathi. Essentials of Medical Pharmacology 2013,7, 798-816
4. James M. Ritter, Flower, Rod,Henderson, Graeme,Loke, Yoon Kong, Macewan, David. Rang
and Dale's Pharmacology. 2016,8,79
5. Williams, David A, and Thomas L. Lemke. Foye's Principles of Medicinal Chemistry.
2002.6,1202–1225.
6. Graham L.Patrick. An Introduction To Medicinal Chemistry.2013,5,468-513
7. V. Alagarsamy Textbook Of Medicinal Chemistry volume ii 2010,399
8. https://en.wikipedia.org/wiki/Antiviral_drug
9. https://bio.libretexts.org/Bookshelves/Microbiology/Book%3A_Microbiology_(Bruslind)/08
%3A_Introdution_to_Viruses
10. https://www.khanacademy.org/science/high-school-biology/hs-human-body-systems/hs-the-
immune-system/a/intro-to-viruses
11. https://www.chemsrc.com/en/cas/144245-52-3_955005.html
12. https://www.researchgate.net/figure/The-HIV-1-life-cycle-and-the-antiretroviral-drug-class-
intervention-points-Entry_fig1_234006451
13. https://www.amboss.com/us/knowledge/Antiviral_agents
14. https://www.drugfuture.com/synth/syndata.aspx?ID=137195
41
44. THANK YOU
Embrace and celebrate the progress
While not letting up the pressure
Until there is a cure.