ANTIVIRAL AGENTS.pptx

ANTIVIRAL AGENTS.pptx

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  ANTIVIRAL AGENTS Farman Ahmad Departmentof pharmaceutical sciences & natural products (cupb)
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  CONTENT •Introduction •Classification •Structure Activity Relationship(SAR)
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  Introduction Anti-viral- Anti=against, Viral=Infectioncaused by Virus Antiviral agents are the drugs which are developed to effectively treat an infection caused by a virus Virus is a submicroscopic infectious agent (pathogen) that replicates only inside living cells Typically a virus consist a segment of nucleic acid(DNA or RNA) surrounded by a protein coat Virus can infect all forms of life from animal and plants to microorganisms
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  CLASSIFICATION Based on Virus:- Non- Retrovirus Anti- Hepatitis HepatitisB Lamivudin Adefovir dipivoxil Tenofovir Hepatitis C Ribavirin Interferon alpha Anti- Influenza Amantadine Rimantadine Oseltamivir Zanamivir Anti- Herpes Idoxuridine Trifluridine Acyclovir Valacyclovir Famciclovir Ganciclovir Valganciclovir Cidofovir Foscarnet Fomivirsen
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  CLASSIFICATION Based on Virus:- Retrovirus Nucleoside reverse transcriptas einhibitors Zidovudine Didanosine Stavudine Lamivudine Abacavir Emtricitabine Tenofovir Non- nucleoside reverse transcriptas e inhibitors Nevirapine Efavirenz Delavirdine Protease inhibitors Ritonavir Atazanavir Indinavir Nelfinavir Saquinavir Amprenavir Lopinavir Entry inhibitor Enfuvirtide CCR-5 receptor inhibitor Maraviroc Integrase Inhibitor Raltegravir
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  CLASSIFICATION Based on ChemicalNature:- Admantane Derivatives:- Amantadine, Rimantadine, Somantadine, Tromantadine. Purine Analogue:- Acyclovir, Ganciclovir, Vidarabine, Valaciclovir, Penciclovir Pyrimidine Analogue:- Trifluridine, Idoxuridine, Zidovudine, Stavudine, Emtricitabine Phosphorus Derivatives:- Foscarnet, Tenofovir Thiazolides:- Nitazoxanide
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  Chemical Structures
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  Mechanism of action:- 1.Purine Analogue
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  Mechanism of action:- 2.Admantane derivatives Inhibit viral replication by blocking the proton channel formed by the M2 protein of influenza A virus. The channel activity is necessary for viral particle un-coating during early and late stages of viral replication.
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  Mechanism of action:- 3.Pyrimidine analogue:- Iodinated thymidine analog, activated intra-cellularly to tri-phosphate which can inhibit DNA polymerases required for incorporation of thymidine into viral DNA. Idoxuridine, instead of thymidine, is incorporated into viral DNA, resulting in faulty DNA and the inability of the virus to infect tissue or reproduce.
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  Structure Activity Relationship(SAR) Acyclovir:- Acyclicside chain at N-9 is essential for anti-viral activity Removal of –CH2OH group from side chain, inactive analogue obtained The 9-alkoxy derivative is highly active against Simplex and Vericella zoster virus, obtained by slight modification at acyl side chain
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  Acyclovir V/S Ganciclovir Ganciclovir differ from acyclovir by a single carboxyl side chain  Ganciclovir 50 times more potent than acyclovir against CMV(Cytomegalovirus) due to absence of thymidine kinase in CMV.  Ganciclovir not require phosphorylation for producing its action against CMV.
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  Acyclovir V/S Vidarabin The use of vidarabine was replaced by acyclovir because of poor solubility and toxicity for herpes simplex virus infection.  The mortality rate was found to be 19% for acyclovir and 50% for vidarabin
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  Acyclovir V/S Penciclovir Penciclovir has a higher affinity for HSV TK than acyclovir  the levels of penciclovir triphosphate in infected cells are much higher than the levels of acyclovir triphosphate
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