Topics in Organic
Chemistry: Modern Medicinal Chemistry (CHEM 515)
Fall 2005
|
Prof. W. P. Malachowski |
Prof. S. A. White |
Class meetings: Tues. and Thurs. 10:00-11:30 AM. All class meetings will be held in PSB 278 unless otherwise noted.
Office Hours: W. Malachowski: Mon. 9:30-10:30 AM, Wed. 4-5:30 PM and by appointment. S. White: Tues. 2-4 PM, Thurs. 11:30-12:30 PM.
Suggested Reference Books (on reserve at Collier Science Library):
General Medicinal Chemistry Topics:
The Organic Chemistry of Drug Design and Drug Action, 1992, by Richard
B. Silverman
An Introduction to Medicinal Chemistry: How Drugs Act and Why, 1997,
Alex Gringauz
Rational Drug Design:
The Organic Chemistry of Enzyme-catalyzed Reactions, 2002, by Richard B.
Silverman
Design of Enzyme Inhibitors as Drugs, 1989, edited by Merton Sandler and H. John Smith
Drug/Generic Name, Mode of Action, Chemical Structure Information:
The Merck Index
Physician’s Desk Reference
Goodman and Gilman’s The Pharmacological Basis of Therapeutics
Tentative Schedule
|
Date (Lecture No.) |
Topic |
Instructor |
|
Aug. 30 (1) |
Introduction/Lead Discovery |
Malachowski/White |
|
Sept. 1 (2) |
Lead Development |
Malachowski |
|
Sept. 6 (3) |
Lead Development |
Malachowski |
|
Sept. 8 (4) |
Molecular Biology and Lead Development: x-ray crystallography, understanding drug resistance and related topics |
White |
|
Sept. 13 (5) |
Quantitative Structure-Activity Relationships (QSAR) |
Malachowski |
|
Sept. 15 (6) |
Development of an H2 histamine antagonist for ulcer treatment: Cimetidine (Tagamet) |
|
|
Sept. 20 (7) |
Development of an H2 histamine antagonist for ulcer treatment: Cimetidine (Tagamet) |
Malachowski |
|
Sept. 22 (8) |
Pharmacokinetics/Drug Metabolism |
Malachowski |
|
Sept. 27 (9) |
Drug Metabolism |
Malachowski |
|
Sept. 29 (10) |
Development of an ACE inhibitor therapy for hypertension treatment: Captopril (Capoten) and Enalapril (Vasotec) |
|
|
Oct. 4 (11) |
Development of an ACE inhibitor therapy for hypertension treatment: Captopril (Capoten) and Enalapril (Vasotec) |
|
|
Oct. 6 (12) |
AIDS treatments: A survey of targets in HIV |
White |
|
Oct. 8-16 |
Fall Break |
|
|
Oct. 18 (12) |
AIDS treatments: A survey of targets in HIV |
White |
|
Oct. 20 (13) |
Develpment of HIV protease inhibitor therapy for AIDS |
Malachowski |
|
Oct. 25 (14) |
Develpment of HIV protease
inhibitor therapy for AIDS |
|
|
Oct. 27 (15) |
Tumor angiogenesis treatment by regulation of gene expression with small, DNA sequence-specific binding molecules |
White |
|
Nov. 1 (16) |
Tumor angiogenesis treatment by regulation of gene expression with small, DNA sequence-specific binding molecules *Mid-term exam distributed today |
White |
|
Nov. 3 (17) |
Tuberculosis Treatment |
Malachowski |
|
Nov. 8 (18) |
Tuberculosis Treatment |
Malachowski |
|
Nov. 10 (19) |
Parasitic Diseases: River Blindness |
White |
|
Nov. 15 (20) |
Malaria |
White |
|
Nov. 17 (21) |
Analgesics: Aspirin and COX-2 inhibitors |
Mary Kim/Stephanie Sarandon |
|
Nov. 22 |
Schizophrenia treatment: Chlorpromazine and ziprasidone |
Ronke Imbeah-Ampiah/Hina Omar |
|
Nov. 24 |
Thanksgiving Break |
|
|
Nov. 29 (22) |
Anti-coagulant treatments: Warfarin and heparin |
Sruti Bhaumik/Darae Ko |
|
Dec. 1 (23) |
Anti-depression treatment: Prozac |
Shadia Bel Hamdounia/Elizabeth Keller/Dustin Raup |
|
Dec. 6 (24) |
Insomnia treatments: melatonin receptor agonists |
Jisun Lee/Andrew Harron |
|
Dec. 8 (25) |
Alzheimer’s Disease: beta-secretase inhibitors |
Marisha Banerji/Anna Merkle |
Exams: One mid-semester take-home exam will be distributed on approximately Nov. 1.
Papers: Students will select an article involving drug development from the scientific literature by Oct. 4 and write a summary (3-5 pages) of the article by Oct. 25.
Student-lead discussions: Students will select an article involving drug development, provide a brief summary of the research and lead a discussion of the work in class.
Final Exam: There will be a take-home final exam distributed at the last class meeting.
Course Grading:
Exam:
100 pts.
Paper: 100 pts.
Presentation:
100 pts.
Final Exam: 150 pts. (x 1)=150 pts.
Total
Points: 450 pts.
Approximate Grading
Scheme: 93-100%
4.0 73-76% 2.0
89-92% 3.7
70-72% 1.7
86-88% 3.3
67-69% 1.3
82-85% 3.0
63-66% 1.0
80-82% 2.7
<63% 0.0
77-79% 2.3
We reserve the right to make modifications to this scheme when I consider it
necessary.
Students with Disabilities: Students who think they may need accommodations in this course because of the impact of a disability are encouraged to meet with me privately early in the semester. Students should also contact Stephanie Bell, Coordinator of Access Services, at 610-526-7351 or sbell@brynmawr.edu, as soon as possible to verify their eligibility for reasonable accommodations. Early contact will help to avoid unnecessary inconvenience and delays.