1. Chemistry 910Practical Medicinal Chemistry Dr John Carran Queen’s University Department of Chemistry

2. Background • In conjunction with Dale Cameron • To develop a course to teach the fundamentals of medicinal chemistry and then to apply them • Lecture component • Practical component

3. Lecture component • Where do drugs act • How do drugs bind • How are drugs metabolised/consequences • How are drugs administered/consequences • How are drugs tested • SAR/QSAR • Molecular modeling (Mike Kuiper, Melbourne, Australia) • Lead compound generation/drug design • Chemistry and improving activity/drug design • Business/intellectual property (Angela Lyon, Parteq, Queen’s University) • Process/scale up • Clinical trials • Case studies

4. Practical component • Aim: To mimic an industrial lead compound selection process. Opiate analgesics. • Each week for 5 weeks a series of compounds with associated data is released. • Each “company” must select one compound to progress in their pipeline to lead compound designation • Each company must rationalise their selection process to a Medicinal Chemistry mentor.

5. Mentors • Dale Cameron - Migenix Corp • Jack Bikker –Wyeth Research • Harold Mastalertz – BMS • Sheldon Hiebert – BMS • Sheldon Crane – Merck Dinesh Vyas Rick Friesen

6. Video conferencing • One per week, weeks 7-11 • Skype or VSee (Free!) • Each “company” has 30 minutes • Questions from mentor on selection process / red herrings • Teaching component • Evaluations on “company” and individual members returned to me

7. “Red Herrings”

8. Sample compound information

9. Course breakdown • Take home assignment (mechanism question in synthesis of Artemisinin) and “midterm” week 6 (handout) (50%) • Videoconferencing assignments (5), weeks 7-11 (25% total) • Professional project report week 9 (5%) • Final poster presentation week 12 (20%)

10. Aims of marked component • Midterm exam- examines lecture component material • Videoconferencing – communication, rationale, comprehension • Report – communication, comprehension • Poster presentation – future work, innovation

11. Current enrollment • Six students • 3 companies (teams) of two students • 5 chemists, 1 pharmacologist • Ideal enrollment 12+ of mixed groups (chemist + pharmacologist + biochemist)

12. Acknowledgements • QCIC • Dale Cameron, Dinesh Vyas, Rick Friesen, Jack Bikker • Harold Mastalertz, Sheldon Hiebert, Sheldon Crane • Angela Lyon, Michael Kuiper • Caitlin Latimer (SWEP program, Queen’s University)