The Latest Process Chemistry you won't find anywhere else...

Medicinal Chemistry

25 - 27 February 2009, Barcelona, Spain

A 3 day course given by
Dr David Clark, Dr David Horwell, Dr Geoff Lawton, Dr Nigel Rogers and Dr Will Watson

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 affects 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 era

Introduction to Medicinal Chemistry, definitions, QSAR studies, drug receptors, Hansch Analysis, physico-chemical properties, Topliss Tree

Physico-chemical properties of drugs. Implications for Absorption.

Lead generation approaches.

Lead generation using computational techniques: molecular recognition, structure- and ligand-based virtual screening, success stories.

Molecular diversity and combinatorial design.

Pharmacokinetics and ADME with examples

Introduction to Lead Optimisation, Case Studies

Overview of some of the reasons for project failure, of safety, in particular to its relationship to chemical structure and of critical issues in Drug Development

Intellectual property issues related to drug discovery

What happens next? - a (very) brief overview of process development issues

 

Course Objectives

At the end of the course, particpants will have gained:

An understanding of how biological disease targets are selected.

An insight in to 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 physiocochemical 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

 

The organisers reserve the right to change the published programme of events and course content as circumstances dictate.