CourseTitle
/
Credit Hours
/
Course No.
/
Prerequisite
/
Year (semester)
/ Lec./Lab. Credit
Medicinal Chemistry 1 /
2
/
0901315
/
0901224
/
2011-2012(1)
/ none
Coordinator Name
/
Lecturer
/
Room No.
/
E-mail
/
Office Hours
Dr. Mutasem Taha
/
Dr. Mutasem Taha
Dr. Adel Ardakani
/

4218

4207

/ / As per lecturer office timetable

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:

  1. 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.

  1. 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.

  1. Subject Specific Skills:

C1) Build solid foundations as a prerequisite topic for as furthur two modules in medicinal chemistry covering most drugs.

  1. 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.

Course Contents :

Week

/ Topics / Topic Details / Reference (chapter) / Assessment
1. / 02-10-2011 / Introduction / Drug Discovery Process / WG1/ F(1-25)
Pat Part C
2. / 09-10-2011 / Physical Properties in Relation to Biological Action
Drug distribution, Protein binding, tissue depots, excretion… / WG2 / F9
Pat Part B
3. / 16-10-2011 / Quiz 1
4. / 23-10-2011
5. / 30-10-2011 / Acid / Base – Partion Coefficient / WG2 / F2 (28)
6. / 06-11-2011 / Expected Eid Vacation
7. / 13-11-2011 / Molecular Modeling / Receptors / WG2(25-30)/ F3
Pat Part B / 1st exam
8. / 20-11-2011 / Isosterism / WG2/ F(47-52)
Pat (222)
9. / 27-11-2011 / Drug-receptor interactions, steric effects, isomerism / F4 + 5 Pat Ch1
10. / 04-12-2011 / Metabolic changes of Drugs and Related Organic Compound pathways, sites and factors affecting drug metabolism / WG3 / F10
11. / 11-12-2011
12. /

18-12-2011

/ 2nd exam
13. /

25-12-2011

/ Prodrugs & Drug latentiation / WG511th ed
Pat Ch14
14 / 01-01-2011 / QSAR, Combinatorial Chemistry, Receptor classifications / WG2 (17-24) Pat 18
15. / 08-01-2011 / Overview of Drug Receptors. A Perspective / F Part II (340)
Pat Part A
16. / 15-01-2011
F I N A L E X A M I N A T I O N 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, 4thed.OxfordUniversityPress, 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 ArdakaniDr. Mutasem Taha

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