Subject to Change
Drug Design PHA 6447
Spring 2012
Course Coordinator: Dr. K.B. Sloan
Phone: 273-7745
Room: P6-33
Time: MWF CG-56 2-4 pm
Description: Outline of how relevant disciplines impact on the development of a new
drug product from the discovery of a new active lead compound to its final refinement as
a commercial product. Contributions of Organic Chemistry, Biochemistry, Metabolic
Chemistry, Physical Chemistry, Analytical Chemistry, and Pharmacological Chemistry
are discussed. The student will gain a general understanding of the drug design process.
Reference Text:
R.B. Silverman, The Organic Chemistry of Drug Action (2004)
Academic Press (Not required)
Date
Lecturer
Jan.
Dr. James
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Holiday
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Dr. James
Dr. Sloan
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Dr. Sloan
Dr. Booth
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Dr. Booth
9
11
13
16
18
20
23
25
27
30
Feb. 1
3
6
8
10
13
15
17
20
22
24
27
29
Mar. 2
5
7
9
12
14
Subject
Metabolism/Toxicology Consideration
Exam
Prodrugs and Soft Drugs
Exam
Drug Design for G Protein-Coupled
Receptors (GPCRs) in the CNS
Exam
Dr. Dunn
Spring Break
↓
↓
Dr. Roth
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1
16
19
21
23
26
28
30
April 2
4
6
9
11
13
16
23
“
Dr. Bergeron
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Dr. Bergeron
Dr. Luesch
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Dr. Luesch
Biochemical/ Mechanism Based
Exam
Natural Products vs High
Throughput Screening
Exam
Learning objectives:
1. Understand the rationale for development of prodrugs or soft drugs.
2. Recognize functional groups that should be masked to obtain specific delivery
objectives.
3. Recognize structural features that provide an opportunity for inserting
metabolically sensitive functional groups.
4. Understand general physiochemical properties that a promoiety should exhibit.
5. To understand from a historical perspective the various ways drugs are
discovered: isolation from natural source, analogue formation, synthesis, etc.
6. To appreciate the need for the continuous effort to discover new drugs.
7. To understand the principles of a “screening program” and the use of various
bioassays.
8. To appreciate the role of “lead compounds” and how they are converted into
useful drugs.
9. To understand why consideration of drug metabolism is important in drug design.
10. To predict types of structural features that are usually metabolically stable and
structural features that usually are susceptible to metabolism.
11. To understand and predict drug interactions that are based on alterations of drug
metabolism.
12. To recognize the importance of stereo selective metabolism in chiral drugs.
13. To familiarize the students with the importance and limitations of the partition
coefficient as a tool in drug design.
14. Understand the structure and function of GPCRs.
15. Understand physiological/anatomical considerations of drug delivery to CNS.
16. Understand pathophysiology and relevant drug targets/strategies for
neurodegenerative and neuropsychiatric disorders.
17. Understand future directions regarding drug discovery/targets for CNS diseases.
18. To assess the role of natural products in drug discovery.
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19. To recognize limitations and advantages of natural products based drug discovery.
20. To become familiar with modern screening methods.
EXAMS AND GRADING:
Format:
The format of the course will involve lectures using combinations of chalk-board
presentations, overhead projection and handouts to deliver the materials.
Evaluation:
The students will be evaluated in five exams each worth 20% of the final 300 points for
the course. They will involve structure, short essay or numerical answers. Old exams
from previous semesters, with correct answers, will be kept on reserve so that students
can anticipate the type and format of exam questions as well as the depth and focus of
particular exams. Students will be allowed to inspect their exams to verify their scores
but exam will be kept by the faculty for 3 years. A key of correct answers for each exam
during the semester will be kept on reserve so that students can determine whether they
have properly applied the processes of induction and deduction to arrive at their answers.
Grading will be on a point basis with >270 (A), >26 (A-), >250 (B+), >240 (B),
>230 (B-), >220 (C+), >210 (C), >200 (C-), >190 (D+), >180 (D), >170 (D-), >170 (E).
There will be no make make-up exams.
Miscellaneous
Class attendance is not mandatory. However, the student will be tested on the lecture
material and in-class handouts which, for the most part, are not covered in precisely the
same way in any available textbook.
Students requesting classroom accommodation must first register with the Dean of
Students Office. The Dean of Students Office will provide documentation to the student
who must then provide this documentation to the Instructor when requesting
accommodation.
Students are expected to complete assignments and take quizzes with integrity. Academic
dishonesty will not be tolerated. If a student commits academic dishonesty, the academic
penalty will be a failing grade in the course. The UF policies and procedures on academic
dishonesty will be followed.
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