Load:
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1. komponenta
Lecture type | Total |
Lectures |
15 |
* Load is given in academic hour (1 academic hour = 45 minutes)
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Description:
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Principles of medicinal chemistry. Receptors and drug action:drug-receptor interactions, ion channels, G-protein-coupled receptors, nuclear receptors, protein kinases, intracellular receptors for gene transcription regulation, antibacterial inhibitors of protein synthesis, enzymes as drug targets. Strategies in drug discovery: natural product as a source for new drugs, existing drugs as a basis for new drugs, disease models as screens for new drugs, rational approach in drug design, bioisosterism, prodrugs.
Development of the most effective drugs. Inhibitors of prostaglandin synthetase: analgetics and antiinflamatorics, inhibitors of angiotensin converting enzyme (ACE): antihipertensive agents, calcium chanel blockers, drugs for the treatment of angina and hypertension, antagonists of histamine receptors (H2) as anti-ulcer drugs, proton pump inhibitors and gastric acid secretion inhibitors, antidepressants based on serotonine modifications, ligands for benzodiazepine receptors: hypnotic, anxiolytic, anticonvulsant and muscle relaxant agents, antagonists of histamine receptors (H1): drugs for the treatment of allergic rhinitis, nucleoside analogues inhibitors of HIV reverse transcriptase as drugs for the treatment of AIDS, fluoroquinolones as antibacterial DNA gyrase inhibitors
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Literature:
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- OBVEZNA LITERATURA:
R. B. Silverman, M. W. Holladay, The Organic Chemistry of Drug Design and Drug Action, 3rd Edition, Academic Press, San Diego, 2014.
C. Wermuth, D. Aldous, P. Raboisson, D. Rognan, Editors: The Practice of Medicinal Chemistry 4th Edition, Academic Press, 2015.
M. Mintas, S. Raić-Malić i N. Raos, Principles of Drug Design, Zagreb, Hinus, 2000.
N. Raos, S. Raić-Malić i M. Mintas, Drugs in the space-pharmacophores and receptors, Školska knjiga, Zagreb, 2005.
- DOPUNSKA LITERATURA:
revijalni članci i znanstvene monografije
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