SCC1092 - SINTESI E PROPRIETA' DELLE SOSTANZE BIOLOGICAMENTE ATTIVE MOD.B

Drug targets: proteins, enzymes and receptors (12 h). Intermolecular binding forces: Protein structure: primary, secondary (alpha-helics, beta turns and beta-sheets) and tertiary. Enzymatic interactions and catalytic role of enzymes. Receptors: neurotransmitters and hormones, receptor activation and signal transduction. Pharmacodynamics and pharmacokinetics (12 h): reversible, irreversible and allosteric inhibitors. Agonists, antagonists and partial agonists, affinity efficacy and potency. Pharmacokinetics: drug absorption, distribution, metabolism and excretion. Drug discovery and development (8 h): choosing a drug target, identifying a bioassay, finding a lead compound. Structure optimization e drug formulation. Preclinical and clinical phases. Antibacterial agents (12 hours). The bacterial cel and mechanisms of antibacterial action. Antimetabolites: sulphonamides. Antibacterial agents which inhibit cell wall synthesis: penicillins, cephalosporins, other -lactam antibiotics(clavulanic acid, carbapenem e monobactams), and glycopeptides. Antibacterial agents which impair protein synthesis: aminoglycosides, tetracyclines, chloramphenicol, macrolides, oxazolidinones. Agents which act on nucleic acid transcription and replication. Antiviral agents (6 hours). Antiviral drugs used against DNA viruses. Antiviral drugs acting against RNA viruses: HIV, flu virus, cold virus, hepatitis C. Drugs acting on the adrenergic nervous system (PNS) (6 hours). Catecholamines: biosynthesis, metabolism and structure activity relationship. Adrenergic agonists: 2-agonists and the treatment of asthma. Adrenergic receptor antagonists: -blockers as cardiovascular drugs. Structure activity relationship of aryloxypropanolamines. Benzodiazepines. The opioid analgesics (4 hours). Morphine: structure-activity relationship. Morphine analogues: drug extension, simplification or drug dissection, rigidification. Morphine antagonists. Anti-ulcer agents (4 hours). Factors influencing the release of gastric acid: Cimetidine and ranitidine. Proton pump inhibitors: Omeprazole.