Chemistry 910 practical medicinal chemistry
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Chemistry 910 Practical Medicinal Chemistry. Dr John Carran Queen’s University Department of Chemistry. 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.

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Chemistry 910 practical medicinal chemistry l.jpg

Chemistry 910Practical Medicinal Chemistry

Dr John Carran

Queen’s University

Department of Chemistry


Background l.jpg
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


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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


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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.


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Mentors

  • Dale Cameron - Migenix Corp

  • Jack Bikker –Wyeth Research

  • Harold Mastalertz – BMS

  • Sheldon Hiebert – BMS

  • Sheldon Crane – Merck

Dinesh Vyas

Rick Friesen


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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




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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%)


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Aims of marked component

  • Midterm exam- examines lecture component material

  • Videoconferencing – communication, rationale, comprehension

  • Report – communication, comprehension

  • Poster presentation – future work, innovation


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Current enrollment

  • Six students

  • 3 companies (teams) of two students

  • 5 chemists, 1 pharmacologist

  • Ideal enrollment 12+ of mixed groups (chemist + pharmacologist + biochemist)


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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)


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