Course Description
The course focuses on fundamental aspects of contemporary medicinal chemistry. The chemical characteristics of drugs and drug targets, pharmaceutical properties of drugs, drug metabolism, principals of pharmacokinetics, pharmacodynamics, toxicology, pharmacogenetics and current methods used in drug design and discovery including 3D QSAR optimization will be discussed in the first half of the class. The second half will focus on applications of these aspects while introducing various drug classes their biochemistry, pharmacology, mechanism of action and toxicity.
Learning Goals and Objectives
The students will be able to apply fundamentals of contemporary medicinal chemistry and understand the processes involved in drug development. The students will also be able to recognize different drug classes and apply the knowledge they gain in this class to their research and future careers.
Course Schedule
| Date | Topic | Instructor |
|---|---|---|
| Jan 4 W | Drug solubility, distribution | Nelson |
| Jan 6 F | Substituent effects, Hammet, Hansch, prodrugs | Nelson |
| Jan 9 M | Drug targets, receptors, etc. | Totah |
| Jan 11 W | Q-SAR and 3D-QSAR | Totah |
| Jan 13 F | Combi, click chemistry, libraries, etc. | Totah |
| Jan 16 M | HOLIDAY - NO CLASS | |
| Jan 18 W | Biotransformation | Totah |
| Jan 20 F | Biotransformation and toxicity | Totah |
| Jan 23 M | Enzyme Kinetics 1 | Kunze |
| Jan 25 W | Pharmacogenetics | Rettie |
| Jan 27 F | Enzyme Kinetics 2 | Kunze |
| Jan 30 M | Antimicrobials | Totah |
| Feb 1 W | Antifungals | Totah |
| Feb 3 F | Antivirals | Totah |
| Feb 6 M | Cholesterol Lowering | Xu |
| Feb 8 W | Cancer 1 | Porubek |
| Feb 10 F | Cancer 2 | Porubek |
| Feb 13 M | Cardiovascular 1 | Atkins |
| Feb 15 W | Cardiovascular 2 | Atkins |
| Feb 17 F | Cholinergics 1 | Nelson |
| Feb 20 M | HOLIDAY - NO CLASS | |
| Feb 22 W | Cholinergics 2 | Nelson |
| Feb 24 F | Cholinergics-AChE | Nelson |
| Feb 27 M | Adrenergics-Parkinsonism | Nelson |
| Mar 1 W | Antihistamines-Proton Pump Inhibitors | Nelson |
| Mar 3 F | Steroids | Nelson |
| Mar 6 M | CNS 1 | Rettie |
| Mar 8 W | Anti-diabetics | Kunze |
| Mar 10 F | CNS 2 | Rettie |
| TBD | MIDTERM EXAM - TBD | |
| TBD | FINAL EXAM - TBD |
Evaluation and Grading
Grading will be based on three take home assignments each worth 100 points applying the concept of medicinal chemistry introduced in the first half of the class. There are two exams each worth 150 points (a midterm and a final) to be arranged outside of class hours. The first midterm will be in class and will cover material from anti-bacterial to cardiovascular 2 to be scheduled during the week of Feb 20th or so. The final exam will be an in class exam on drug topics not covered in the midterm scheduled during finals week.
Suggested Textbooks
The faculty will provide handouts for the class with their notes; however, the texts below are recommended for further reading and reference.
- Richard B. Silverman and Mark W. Holladay. The Organic Chemistry of Drug Design and Drug Action, 3rd Ed., Elsevier Academic Press, London (2014).
- Li Di and Edward Kerns, Drug-like properties: Concepts, structure design and methods, Academic Press, London, 2016
- D.A. Williams and T.L. Lemke. Foye's Principles of Medicinal Chemistry, 7th Ed., Lippincott Williams and Williams, NY (2012).
- J.H. Block and J.M. Beale, Jr. Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry, 12th Ed., Lippincott-Raven, NY (2010).