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In-House Training

Medicinal Chemistry

Tutors: Dr John Studley Dr David Clark Dr Martin Swarbrick Dr Rachael White Dr Paul Beswick

Medicinal chemists need to understand the relationship between chemical structure and the physical properties of molecules and how this translates into compound stability and the interaction of the molecule with biological structures.  These biological targets include proteins, lipids, nucleic acids and cell membranes.  Interaction of the molecules with these targets affects the distribution of the compound in biological systems and modulates biological function.

To do this successfully the medicinal chemist needs to be aware of how target selection is carried out and how this effects lead generation.  The medicinal chemist needs knowledge of structure property relationships, the physico-chemical properties of drugs and how these molecules interact with the body– pharmacokinetics and ADME (Absorption, Distribution, Metabolism and Excretion).

The course also includes an overview of the use of computational chemistry in virtual screening and library design.  The lectures are backed up by a number of case studies and tutorial sessions, which involve the participants in using the concepts discussed.

Course Outline

Introduction: Overview of drug discovery process, target selection in the post-genomic eraIntroduction to Medicinal Chemistry, definitions, QSAR studies, drug receptors, physico-chemical propertiesPhysico-chemical properties of drugs, and implications for AbsorptionLead generation approachesLead generation using computational techniques: molecular recognition, structure- and ligand-based virtual screening, success storiesMolecular diversity and combinatorial designPharmacokinetics and ADME, with examplesIntroduction to Lead Optimisation, Case StudiesOverview of some of the reasons for project failure, of Safety, in particular to its relationship to chemical structure and of critical issues in Drug DevelopmentIntellectual property issues related to drug discoveryWhat happens next? – a (very) brief overview of process development issues

Benefits of Attending

  • An understanding of how biological disease targets are selected.
  • An insight into the terms, definitions and analysis methods used by
    medicinal chemists in the pharmaceutical industry.
  • An introductory knowledge of Pharmacokinetics and ADME
    (Absorption, Distribution, Metabolism and Excretion) and how
    physicochemical properties influence absorption.
  • An introduction to the use of computational chemistry including
    pharmacophore generation, virtual screening and library design.
    An overview of safety assessment and how chemical structure
    relates to safety.




Who Should Attend

  • Young chemists who have just started in industry as medicinal chemists.
  • Experienced medicinal chemists who wish to gain additional knowledge on how to obtain compounds with optimal drug-like properties and get up to date with the latest thinking.
  • Chemists from other areas of Research and Development who would like to gain an appreciation of the processes and drivers involved in drug discovery.
  • Students who are planning a career in industry and can obtain company sponsorship

What's Included

The course fee includes:

  • comprehensive course manual
  • coffee/tea refreshments breaks throughout each day
  • buffet lunch each day
  • course dinner on the first evening
  • course certificate
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