Syllabus
CHEM4120
Organic Chemistry of Drug Design and Drug Action
Spring, 2016
Professor: Robert S. Phillips
9:05 AM MWF, Rm. 453
Text: "The Organic Chemistry of Drug Design and Drug Action”, 3rd Ed., Richard
B. Silverman
Date
Jan. 11 Ch. 1, Introduction; Case history: Ergot
Jan. 13 Ch. 1, Introduction
Jan. 15 Ch. 2, Lead Discovery and Lead Modification; Kynurenine Pathway;
Human morphine
Jan. 18 MLK Jr. holiday
Jan. 20 Ch. 2, Lead Discovery and Lead Modification
Jan. 22 Ch. 2, Lead Discovery and Lead Modification; Linear free energy
relationships
Jan. 25 Ch. 2, Lead Discovery and Lead Modification; Hansch π-values
Jan. 27 Ch. 2, Lead Discovery and Lead Modification
Jan. 29 Ch. 2, Lead Discovery and Lead Modification
Feb. 1 Ch. 2, Lead Discovery and Lead Modification, Problems 3, 5, 7, 8, 10, 11,
17, 21, 24, 25; Recently approved drugs, Total number of drugs
Feb. 3 Ch. 3, Receptors; Structure of a G-protein coupled receptor; Halogen
bonding
Feb. 5 Ch. 3, Receptors; Functional selectivity in receptors
Feb. 8 Ch. 3, Receptors
Feb. 10 Ch. 3, Receptors
Feb. 12 Ch. 3, Receptors, Problems 1-11
Feb. 15 Ch. 4, Enzymes; Catalytic power of enzymes
Feb. 17 Ch. 4, Enzymes
Feb. 19 Ch. 4, Enzymes
Feb. 22 Ch. 4, Enzymes, Problems 2,3,5,7,10,11,13,14
Feb. 24 Midterm Exam, Ch. 1-4
Feb. 26 Ch. 5, Enzyme Inhibition and Inactivation; Case History Calabar;
Transition state analogue inhibitors
Feb. 29 Ch. 5, Enzyme Inhibition and Inactivation; Design of a cholinesterase
inhibitor
Mar. 2 Ch. 5, Enzyme Inhibition and Inactivation
Mar. 4 Ch. 5, Enzyme Inhibition and Inactivation; Pharmacogenomics--Warfarin
Mar. 7-11, Spring break
Mar. 14 Ch. 5, Enzyme Inhibition and Inactivation
Mar. 16 Ch. 5, Enzyme Inhibition and Inactivation; Problems 2, 5, 6, 8, 9, 11, 13,
14, 15; Designer Drugs
Mar. 18 Ch. 6, DNA-Interactive Agents
Mar. 21 Ch. 6, DNA-Interactive Agents
Mar. 23 Ch. 6, DNA-Interactive Agents; Problems 2, 5, 7, 8, 9, 10, 11, 14;
Ribosomal inhibitors
Mar. 25 Ch. 7, Drug Resistance and Drug Synergism
Mar. 28 Ch. 7, Drug Resistance and Drug Synergism
Mar. 30 Ch. 7, Drug Resistance and Drug Synergism
Apr. 1 Ch. 7, Drug Resistance and Drug Synergism; Problems 1-8
Apr. 4 Ch. 8 , Drug Metabolism; Wohler: discovery of hippuric acid
Apr. 6 Ch. 8, Drug Metabolism
Apr. 8 Ch. 8, Drug Metabolism
Apr. 11 Ch. 8, Drug Metabolism; Problems 2, 3, 4, 7, 9, 11, 13
Apr. 13 Ch. 9, Prodrugs and Drug Delivery Systems
Apr. 15 Ch. 9, Prodrugs and Drug Delivery Systems
Apr. 18 Ch. 9, Prodrugs and Drug Delivery Systems
Apr. 20 Ch. 9, Prodrugs and Drug Delivery Systems; Problems 1, 3, 4, 5, 7, 10, 12,
15
Apr. 22 Class presentations
Apr. 25 Class presentations
Apr. 27 Class presentations
Apr. 29 Class presentations
May 2 Class presentations
Wednesday, May 4, 8:00-11:00 AM Final Exam
The course syllabus is a general plan for the course; deviations announced to the
class by the instructor may be necessary. The grade for this course will be
composed of a midterm exam counting 30%, a written report and short class
presentation on a drug of your choice, counting 30%, class attendence grade of
10% (two short unannounced quizzes), and a final exam counting 30%. I do not
think that it will be necessary to “curve” the grades in this course.
Office hours: MWF 10-11, TH 9-10
All academic work must meet the standards contained in “A Culture of Honesty.”
Students are responsible for informing themselves about those standards before
performing any academic work.
A printable copy of this syllabus can be downloaded from this link.
The
course
evaluation
can
be
done
online
at
https://webapps.franklin.uga.edu/evaluation/. The evaluation will be open until the
end of the day on April 30. Students who fill out the course evaluation will receive
a bonus of 2% on their final course average. I will not see the comments or scores
until after grades have been submitted.