Download - Applied Science University

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.
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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
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