Medicinal Chemistry Pharmacy 621 (34080)
TTh 12:00-2:00; Skaggs 270
Prof.
C. M. Thompson, x4643, charles.thompson@umontana.edu
Textbook
(required):
An
Introduction to Medicinal Chemistry, 2nd Edition, Graham L. Patrick, Oxford
University Press, 2001; paper, ISBN 0198505337, approximately $ 43.95.
Suggested
Support Texts:
Delgado, J and Remers, W., "Textbook of Organic Medicinal and
Pharmaceutical Chemistry," Lippincott-Raven, Philadelphia, 1998 (more drug
pharmacology). Undergraduate organic and biochemistry texts.
Ancillary
reading:
Various reading assignments will be assigned from the primary literature. The
journals are: Bioorganic and Medicinal Chemistry Letters, Bioorganic and
Medicinal Chemistry, European Journal of Medicinal Chemistry & The
Journal of Medicinal Chemistry.
Meeting
time(s): Lectures on Tuesday 12:00-2:00 and Thursday
12:00-1:00. Discussion of primary
literature paper on Thursday from 1:00-2:00.
Course Aims: The aim of the class is to introduce graduate and upper level undergraduate students to the main theoretical, experimental and philosophical concepts that define medicinal chemistry. A second aim is familiarize students with the primary literature in Medicinal Chemistry and to develop critical method to analyze the literature in Medicinal Chemistry. Upon completion of this course, the student should have a better understanding of how and why certain chemicals interact at biological targets. The range of material is split into: (a) basic principles and techniques and (b) select topic areas in medicinal chemistry. These two topic areas will be complemented by coverage of the primary literature. To help you through the course, I will make many of the lecture notes and structures electronically available. This is not a memorization course - the emphasis is on understanding relationships between chemical structure and the biological mode of action.
What
I expect: (a) good attendance, (b) keeping up with
reading assignments, (c) feedback on literature articles = participation, (d)
professional preparation and planning (don't wait till the last minute to read
the assignments!) and (e) a growing appreciation of the interdisciplinary
nature of medicinal chemistry.
Grading: The letter
grade will be assigned based upon performance in the following areas:
Quiz 1 100
Quiz 2 100
Quiz 3 100
} any two best
Final Exam 50
Review/Participation on Literature
Articles 250
Total (max) 500 pts
Only your two best quiz
scores will count toward your grade.
The quizzes will cover material up until the prior lecture (not intended
to be comprehensive) and may include literature articles. If you miss a quiz, it counts as your lowest
score. The final exam will be
comprehensive emphasizing key points or concepts. Each student will receive a score of 0 to 25 for each paper we
cover in Thursday’s journal article review (total 250 pts).
You will need
Adobe Acrobat reader to open the electronic notes and articles (will be
uploaded January 21st).
|
Date |
Day
|
Lecture Title (tentative) |
Notes (*.pdf) |
Reading (Graham) |
Article or Quiz |
|
Jan 27 |
T |
Introduction
to Med Chem; Org Functional Groups |
|
|
|
|
Jan 29 |
Th |
Review
of Protein Structure |
20-35 |
||
|
Feb 3 |
T |
Drug
Action at Enzymes |
|
37-64 |
|
|
Feb 5 |
Th |
Drug
Action at Enzymes |
37-64 |
||
|
Feb 10 |
T |
Drug
Action at Receptors |
|
66-92 |
|
|
Feb 12 |
Th |
Drug
Action at Receptors |
66-92 |
||
|
Feb 17 |
T |
Receptor
Structure |
|
94-120 |
|
|
Feb 19 |
Th |
Receptor
Structure & Signal Transduction |
|
Quiz 1 |
|
|
Feb 24 |
T |
Nucleic
Acid Structure and DNA Drugs |
|
123-141 |
|
|
Feb 26 |
Th |
Drugs
Used to Treat Cancer |
|
||
|
Mar 2 |
T |
Drug
Discovery & Drug Targets |
|
142-169 |
|
|
Mar 4 |
Th |
Drug
Targets and Drug Development |
|
||
|
Mar 9 |
T |
Structure
Activity & QSAR |
|
169-177 |
|
|
Mar 11 |
Th |
Structure
Activity & QSAR |
258-279 |
||
|
Mar 16 |
T |
Structure
Activity & QSAR |
|
|
|
|
Mar 18 |
Th |
Drug
Design & Substituent Variation |
191-206 |
Quiz 2 |
|
|
Mar 23 |
T |
Pharmacokinetics |
|
|
|
|
Mar 25 |
Th |
Pharmacokinetics |
|
||
|
Mar 30 |
T |
SPRING
VACATION – No Classes |
|
|
|
|
Apr 1 |
Th |
SPRING
VACATION – No Classes |
|
|
|
|
Apr 6 |
T |
Solid
Phase and Combinatorial Synthesis |
|
289-317 |
|
|
Apr 8 |
Th |
Solid
Phase and Combinatorial Synthesis |
|
||
|
Apr 13 |
T |
Antibacterial
Agents |
|
|
|
|
Apr 15 |
Th |
Antibacterial
Agents |
|
||
|
Apr 20 |
T |
Cholinergic
and Adrenergic Drugs |
432-479 |
|
|
|
Apr 22 |
Th |
Adrenergic
Drugs |
|
||
|
Apr 27 |
T |
Serotonergic
or Glutamatergic Drugs |
|
|
|
|
Apr 29 |
Th |
Opiates |
511-548 |
Quiz 3 |
|
|
May 4 |
T |
to
be announced |
|
|
|
|
May 6 |
Th |
to
be announced |
|
|
Review |
|
|
|
|
|
|
|
|
Final |
|
|
|
|
FINAL |