Předmět Princip. of antic. and antiv. drug d.II. (UCH / 646)

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Materiál	Typ	Datum	Počet stažení

Obsah

Contents of lectures:1.Base-modified nucleoside inhibitors of polymerases. Active antimetabolites. Acyclic nucleoside analogs. Acyclovir, Ganciclovir. Herpesvirus thymidine kinase. Foscarnet and analogs of inorganic diphosphate.2.ANP, their principle, syntheses and activity of HPMP-derivatives.3.Chelating agents. Pol protein inactivating disulphides. Sugar-modified (azido, dideoxy, didehydro, amino) nucleosides as inhibitors of reverse transcriptase. Chain terminators. Chemotherapy of AIDS and hepatitis B. Adefovir, tenofovir.4.Covalent interaction with DNA. Alkylation agents, nitrogen mustards, nitrosoureas. Cis-platinum and related compounds as alkylation agents. Targeted antitumor drugs based on transformation of prodrugs in the reductive medium of tumor cells. Thymidine phosphorylase inhibitors. Inhibitors of angiogenesis.5.Non-covalent intractions with DNA and RNA. Intercalators. Cancerogenicity of polyaromatic coponds. Topoisomerases and their inhibitors. Ellipticin. Mitomycins. Bleomycins and radiomimetic mechanism of DNA chain cleavage.6.Inhibitors of proteosynthesis, puromycin antibiotics, gougerotin. Prodrugs. Hydrophilic modification, nucleotide prodrugs. Chirality at phosphorus atom.7.Non-nucleoside inhibitors of reverse transcription. Inhibitors of viral proteases (Asp, Ser). AIDS chemotherapy. Posttranslation modification: methylation, glycosylation, polyadenylation, prenylation. Capping. Analogs of SAM, SAH. SIBA. Farnesylation.8.Glycosylation inhibitors I. Deoxynojirimycins, 2-deoxyglucose. Aromatase and inhibitors of hormone-activated tumors. Inhibitors of 5?-reductase. Cell apoptosis. Telomerase inhibitors. ADP-translocase and mitochondria.9.Ado-receptors and P2 receptors. Syntheses of purinoceptor antagonists. Membrane transport. Immunomodulators. Antisense oligonucleotides. Principles of chemical synthesis of oligonucleotides. Phosphothioates. Analogs of cAMP. Oligonucleotides as interferon inducers. Toll-like receptors. Glycosythransferase inhibitors II.10. Methods of in vitro a in vivo screening. Embryotoxicity. Drug development. Drug formulations. Preclinical and clinical trial phases. Placebo. GLP, GMP. Novel drug approval process (FDA, EMEA, SUKL). Patent protection of novel drugs.

Literatura

R. B. Silverman: The Organic Chemistry of Drug Design and Drug Action, Academic Press, 2nd edition.