SCIE 682
Drug Discovery

Robert DeSimone      

Course Schedule
Session 1 Introduction: Introduction to Medicinal Chemistry

Discover Time Line
Clinical Time Line
Economics of Drug Development
Risk vs. Reward
Top Ten List (best selling compounds)
New Compounds on the Market

Session 2 Medicinal Chemistry Concepts

Receptor Theory:
Binding Assays
Functional Assays

Structure Activity Relationships
Metabolism (ADME)
Lipinski Rule of Five

Session 3 Treatment of Anxiety

Use of Benzodiazepines
New Approach to Anxiety Treatment
GABAa Receptor/Subtypes

Session 4 Treatment of Anxiety Continued

Cognition Enhancement
Senile Dementia

Session 5 New Approach to Drug Design

Combinatorial Chemistry
Solid vs. Solution Phase Synthesis
Conserved Binding Motif
Virtual Library

Session 6 New Approach to Drug Design Continued

Computational Chemistry
High Throughput Screening
Screening of Virtual Library

Session 7 Treatment of Cardiovascular Diseases

Diuretics
B-blockers

Session 8 Treatment of Cardiovascular Diseases Continued

Rennin Angiotensin
Calcium Channel Blockers

Session 9 Treatment of Diabetes

Insulin
GLP-1
Somatostatin

Session 10 Anticancer Drugs
Session 11 Analgetics and Nonsteroidal Antiinflamatory Agents
Session 12 Project Presentations
Session 13 Project Presentations
Office Hours: before or after class or by appointment
Grading:
Homework/Class Discussions:     20%
Midterm (open book take home exam):     40%
Final Project on Drug Discovery of the student's choice:    40%
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