Medicinal Chemistry

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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 Objectives

This course in medicinal chemistry sets out to train organic chemists to understand the key factors in discovering a new drug substance, from target selection, through lead generation and lead optimisation, to the selection of a development candidate. The course will cover aspects of the drug discovery process such as structure activity relationships, the use of computational chemistry in drug discovery, ADME and safety issues.

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

At the end of the Course, participants will have gained

• 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 the 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 of chemical structure and safety

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