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Applied Science University Faculty: Pharmacy Department: Pharmaceutical Chemistry & Pharmaconosy ( Course Syllabus ) CourseTitle Medicinal Chemistry 1 Coordinator Name Dr. Mutasem Taha Credit Hours 2 Lecturer Dr. Mutasem Taha Dr. Adel Ardakani Course No. 0901315 Room No. 4218 4207 Prerequisite 0901224 E-mail Year (semester) 2011-2012 (1) Lec./Lab. Credit none Office Hours As per lecturer office timetable [email protected] Course Objectives: To be able to discuss and explain the effects of drug structure and physicochemical properties on pharmacokinetics (drug absorption, distribution, metabolism and excretion), pharmacodynamics (reaction of drug with respective receptor), drug latentiation (prodrugs) and drug metabolism (chemical modifications performed by the host bio-system on the drug molecules). Course Description: Following the basic knowledge in organic chemistry and physical pharmacy, medicinal chemistry 1 will introduce the student to the expected effects of active organic molecules inside the human physiological system to be able to predict physicochemical properties of these active ingredents. As well as the expected metabolic routes for them. Also an introduction to he drug discovery process including QSAR and computer based studies will be covered. Intended Learning Outcomes : Successful completion of this course should lead to the following learning outcomes: A. Knowledge and understanding: A1) To be able to discuss physicochemical properties of active ingredients. A2) To be predict qualitatively pharmacokinetic properties from molecular structures. A3) To be able to illustrate theoretical aspects dealing with modern drug discovery, including quantitative structure-activity relationship A4) To show an uderstanding of the prodrug concept and its useful applications. A5) To be able to predict the outcomes of different metabolic routes for a general medicinal compounds. B. Intellectual skills: B1) Apply general organic reactions for the synthesis and application of prodrug units. B2) Apply general organic chemistry and physical pharmacy in predicting the physicochemical properties of active ingredients. B3) Apply some QSAR techniques for drug discovery based on computer models. C. Subject Specific Skills: C1) Build solid foundations as a prerequisite topic for as furthur two modules in medicinal chemistry covering most drugs. D. Transferable Skills: D1) Combine the knowledge from chemistry, physical pharmacy, physiology and biology to understand and then to predict the behavior of active ingredients in living tissue. D2) Utilize basic general knowledge as sources for new chemical entities which are the starting point in the drug discovery process. 1 Course Contents : Week 1. Topics 02-10-2011 2. 09-10-2011 3. 16-10-2011 4. 23-10-2011 5. 30-10-2011 6. 06-11-2011 7. 13-11-2011 8. Introduction / Drug Discovery Process Physical Properties in Relation to Biological Action Drug distribution, Protein binding, tissue depots, excretion… WG2 / F9 Pat Part B Acid / Base – Partion Coefficient WG2 / F2 (28) 27-11-2011 10. 04-12-2011 11. 11-12-2011 12. 18-12-2011 13. WG2(25-30)/ F3 Pat Part B WG2/ F(47-52) Pat (222) Molecular Modeling / Receptors Isosterism Drug-receptor interactions, steric effects, isomerism F4 + 5 Pat Ch1 Metabolic changes of Drugs and Related Organic Compound pathways, sites and factors affecting drug metabolism WG3 / F10 25-12-2011 Prodrugs & Drug latentiation 14 01-01-2011 QSAR, Combinatorial Chemistry, Receptor classifications 15. 08-01-2011 16. Assessment Quiz 1 Expected Eid Vacation 20-11-2011 9. Reference (chapter) WG1/ F(1-25) Pat Part C Topic Details F Part II (340) Pat Part A 15-01-2011 EXAMINATION 2nd exam WG5 11th ed Pat Ch14 WG2 (17-24) Pat 18 Overview of Drug Receptors. A Perspective FINAL 1st exam W EE K Course quality improvement : includes Medicinal labs 2 and 3 include chemical drawing and molecular modeling experiments. Animations are provided from the Power Point slides from Graham Patrick book's website. Grade Distribution : Assessment Grade Date - First Exam 23 TBD - Second Exam 25 TBD - Assignments 2 TBD - Final Examination 50 TBD * Make-up exams will be offered for valid reasons. It may be different from regular exams in content and format. Reading List: Text Books WG: Wilson and Gisvold’s Textbook of Organic Medicinal and Pharmaceutical Chemistry, by Wilson, Beale, Block, and Gisvold, 12th ed. Lippincott Williams & Wilkins, ISBN: 9780781779296. 2010 F: Foye's Principles of Medicinal Chemistry, by Lemke and Williams, 6th ed. Lippincott Williams & Wilkins, ISBN: 9780781768795. 2008 Other References An Introduction to Medicinal Chemistry, by Graham Patrick, 4th ed. Oxford University Press, USA; ISBN: 9780199234479. 2009 Medicinal Chemistry: An Introduction, by Garth Thomas, 2nd ed. John Wiley & Sons, ISBN: 9780470025987. 2008 Last updated on 16 / 9 / 2011 by: Dr. Adel Ardakani & Dr. Mutasem Taha 2