Learning Outcomes
This course is concerned with the discovery, design, synthesis and identification of biologically active compounds acting on the central nervous system (CNS), antiepileptics drugs: miscellaneous anticonvulsants, miscellaneous antiparkinson agents, NMDA receptor antagonists for the treatment of Alzheimer’s disease, antimigraine agents, agonists/antagonists of Αdenosine, Inhibitors of adenyl-cyclase- Inhibitors of PDEs, Μethylphenidate and analogues, Inhibitors of serineproteases, Statines, Αgonists/Αntagonists of CCK. Quantitative structure-activity relationships (SAR/QSAR). Finally, agents used illegally, such as opioids, cannabinoids and other drugs of addiction, with special pharmaco-sociologic interest, are studied.
Aims are the critical knowledge and thorough examination of synthesis, structure, correlation of structure with drug action, fate of the drugs in the organism, sites of loss, therefore duration of drug action. Aim is also to familiarise the students with relations governing molecules acting on CNS and the central nervous system site of action, as well as the involved neurotransmitters.
Scills: By the end of this course, the students should be able to: Know the synthesis of the important drug molecules used for pathologic conditions concerning CNS and cardiovascular system, the physical and chemical properties of these drugs, the biological properties that give the therapeutic potential to these groups of drugs, the structural changes (i.e. metabolism) and fate of these molecules in the organism, the duration of action, the possibility of biodetoxication or biotoxication. Reach conclusions on the relationships between action and structural and physicochemical characteristics and examples are studied of characteristic molecules used illegally as narcotic and addictive agents, from the pharmacochemical point of view.
Course Content (Syllabus)
1) Eleni A. Rekka
Τhis course analyses synthetic pathways, extraction-isolation, physical, chemical, biological properties, purity and quality control, identification, quantitative determination, molecular mode of action, side effects, fate in the organism - drug metabolism, structure-activity relationships, therapeutic uses, adverse actions and doses of drugs acting on the Central Nervous System, i.e. hypnotics, anxiolytics, neuroleptics (drugs acting against mania and psychoses), antidepressants. Opioids and other centrally acting analgesic and antitussive agents. Opioid antagonists. Introduction to addiction. Agents used in detoxication and addiction therapy. Cannabinoids, psychotoxic and psychedelic drugs.
2) Ioannis Nicolaou
Pharmacochemical approach (as design, synthesis, physicochemical properties, target cell interactions, structure-activity relationships, pharmacochemical interpretation of toxicity, metabolism) of the below classes of drugs: miscellaneous anticonvulsants, miscellaneous antiparkinson agents, NMDA receptor antagonists for the treatment of Alzheimer’s disease, antimigraine agents.
3) Dimitra Hadjipavlou-Litina
Stimulants-Αnaleptics -Agonists/antagonists of Αdenosine, Inhibitors of adenyl-cyclase- Inhibitors of PDEs, Μethylphenidate and analogues, Inhibitors of serineproteases, Statines, Αgonists/Αntagonists of CCK. Quantitative structure activity relationships (SAR/QSAR). Examples of Quantitative structure activity relationships determination and chemical identifications.
Additional bibliography for study
1) Ελένη Ρέκκα
• A. Korolkovas, “Essentials of Medicinal Chemistry”, Wiley International Publications, John Wiley & Sons, 2003.
• J.M. Beale, J. Block, “Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry”, Lippincott Williams & Wilkins; 12th ed., 2010
2) Ιωάννης Νικολάου
• Journal of Medicinal Chemistry (ACS Publications)
• Bioorganic & Medicinal Chemistry Letters - Elsevier
• Bioorganic & Medicinal Chemistry (ISSN 0968-0896)
• The Journal of Biological Chemistry
• Chemical Research in Toxicology (ACS Publications)
• Drug Metabolism and Disposition
3) Δήμητρα Χατζηπαύλου-Λίτινα
• Medicinal Chemistry Principles and Practice, Ed. F.D.King. 1994, The Royal Society of Chemistry, ISBN 0-85186-494-5
• Contemporary Drug Synthesis Li J.J, Johnson D., Sliskovic D., Roth B. Wiley-Interscience,2004, ISBN 0-471-21480-9
• New Trends in Synthetic Medicinal Chemistry, Ed. F. Gualtieri, Wiley –VCH, Vol. 7, 2000
• Annual Reports in Medicinal Chemistry, Academic Press
• Journal of Medicinal Chemistry (ACS Publications)
• Bioorganic & Medicinal Chemistry Letters - Elsevier
• Bioorganic & Medicinal Chemistry (ISSN 0968-0896)
• “Practical Pharmaceutical Chemistry part I, II) The Athlone Press 1975
• “Principles of Medicinal Chemistry” W.O. Foye, ed. Lea & Febiger, 1995
• “Remington’s Pharmaceutical Sciences”, Osol A. ed. Mack Publishing Co., 1980
• « Goodman & Gilman’s The Pharmacological Basis of Therapeutics » Goodman a., Hardman J., Limbird L., eds MacMillan Publishing Co 2001
• “Strategies for Organic Drug Synthesis and Design” Lednicer, D., ed. Wiley J. & Sons 2000
• ”Essentials of Pharmacology” Theocharidis T. Little, Brown & Company 2nd edition, 1999
• Drug Actions, Basic Principles and Therapeutic Aspects, Mutschler/Devendorf
• Archiv.Pharm 317, 183-185, 1984
• Arch Pharm 325, 483-90, 1992.
• Arch Pharm 328, 689-698, 1995
• Intensive Care Med. 18, 449-454, 1992
• Greenblatt et al. (1999) FEBS Letters 463, p321
• Dvir et al. (2003) JACS 125, p363
• Bar-On et al. (2002) Biochemistry 41, p3555.
• Kryeger et al.,(1997) Structure 7,297
• Raves et al. (1997) Nature Structural Biology 4, p57
• Εθνικό Συνταγολόγιο 2007, Εθνικός Οργανισμός Φαρμάκων