Class meetings:
Tues. and Thurs. 11:40-1:00 PM.
All class meetings will be held in PSB 278 unless otherwise noted.
Office Hours: Mon. 9:30-10:30 AM, Th. 3-4:30 PM and by appointment
Suggested Reference Books:
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, 2000, by Richard B. Silverman
Design of Enzyme Inhibitors as
Drugs, 1989, edited by Merton Sandler and H. John Smith
Solid-Phase and Combinatorial Chemistry
Topics:
Solid-PhaseSynthesis and Combinatorial
Technologies, 2000, by Pierfausto Seneci
A Practical Guide to Combinatorial
Chemistry, 1997, edited by Anthony W. Czarnik and Sheila H. DeWitt
Tentative Schedule
| Date (Lecture No.) | Topic |
| Sept. 4 (1) | Introduction/Drug Discovery |
| Sept. 6 (2) | Drug Development |
| Sept. 11 (3) | Drug Development |
| Sept. 13 (4) | Drug Metabolism |
| Sept. 18 (5) | Rational Drug Design withProteaseInhibitors:Introduction |
| Sept. 20 (6) | Angiotensin Converting Enzyme Inhibitors |
| Sept. 25 (7) | Matrix Metalloprotease Inhibitors |
| Sept. 27 (8) | Renin Inhibitors |
| Oct. 2 (9) | HIV Protease Inhibitors |
| Oct. 4 (10) | Human Leukocyte Elastase and Thrombin
Inhibitors
*Select literature article for paper on rational drug design by today |
| Oct. 9 (11) | Cysteine Protease Inhibitors |
| Oct. 11 | Exam 1 |
| Oct. 15-19 | Fall Break |
| Oct. 23 (12) | Rational Drug Design with Other Enzymes: Cyclooxygenase-2 and HMG-CoA Reductase Inhibitors |
| Oct. 25 (13) | Open |
| Oct. 30 (14) | Open
*Papers due today |
| Nov. 1 (15) | Solid-Phase Organic Synthesis: Introduction |
| Nov. 6 (16) | Resins and Linkers |
| Nov. 8 (17) | Reactions |
| Nov. 13 (18) | Protection Strategies |
| Nov. 15 (19) | Reaction Analysis |
| Nov. 20 | Exam 2 |
| Nov. 27 (20) | Synthesis of Oligomeric Structures |
| Nov. 29 (21) | Synthesis of Small Organic Molecules |
| Dec. 4 (22) | Combinatorial Chemistry: Introduction |
| Dec. 6 (23) | Combinatorial Library Synthesis |
| Dec. 11 (24) | Student Presentations |
| Dec. 13 (25) | Student Presentations |
Exams: Two in-class semester exams will be given on the dates noted in the schedule.
Papers: Students will select an article involving rational drug design from the scientific literature by Oct. 4 and write a summary (3-5 pages) of the article by Oct. 30.
Presentations: Students will select an article involving solid-phase organic synthesis or combinatorial chemistry and deliver a 20 minute presentation on the article to the class.
Final Exam: There will be a two-hour self-scheduled final exam without lecture notes, textbook or any other associated course materials.
Course Grading:
Exams:
100 pts. (x 2)=200 pts.
Paper:
100 pts.
Presentation:
100 pts.
Final Exam:
150 pts. (x 1)=150 pts.
Total Points: 550 pts.
Approximate Grading
Scheme: 95-100% 4.0
73-76% 2.0
90-94% 3.7 70-72%
1.7
87-89% 3.3 67-69%
1.3
83-86% 3.0 63-66%
1.0
80-82% 2.7 <63%
0.0
77-79% 2.3
I reserve the right to make modifications
to this scheme when I consider it necessary.
Students with Disabilities: Any student eligible for and needing academic adjustments or accommodations because of a disability is requested to speak with me within the first two weeks of class.