Medicinal Chemistry
Short course
In Mayfield
Description
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Type
Short course
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Location
Mayfield
At the end of the course, participants 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 physicochemical properties influence absorption. An introduction to the use of computational chemistry including pharmacophore generation, virtual screening and library design. Suitable for: 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 druglike 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.
Facilities
Location
Start date
Start date
Reviews
Teachers and trainers (5)
Dr David Clark
Director of Computer-aided Drug Design (CADD) and Information Services
Dr David Clark is Director of Computer-aided Drug Design (CADD) and Information Services and was a founding scientific team member of Argenta Discovery in 2000. David began his career working for Proteus Molecular Design for 3 years where he was involved in developing software for de novo ligand design and protein-ligand docking. He then spent 4 years working in the CADD group of Aventis/Rhone-Poulenc Rorer before joining Argenta. David is a graduate of the University of Oxford where he studied chemistry. ...
Dr David Horwell
London University
Dr David Horwell graduated from London University before undertaking his PhD in organic heterocyclic chemistry at Leicester University with Professor C W Rees, CBE, FRS. He then carried out post-doctoral research in Canada (National Research Council, Ottowa), Florida (Gainesville) and at Imperial College, London. This was followed by a research career in the pharmaceutical industry with Eli Lilly, Parke-David, Warner-Lambert and Pfizer. ...
Dr Geoff Lawton
Vice President Chemistry and Preclinical Sciences at Roche Bioscience
Dr Geoff Lawton was formerly the Vice President Chemistry and Preclinical Sciences at Roche Bioscience, Palo Alto, California and has extensive experience of new medicine discovery and early development. In 2001 he became an independent consultant in all aspects of drug discovery from target identification, through lead finding and optimisation to drug candidate selection and evaluation. He is currently Research Director at Lectus Therapeutics. ...
Dr Nigel Rogers
Director of Pre-clinical Science at Roche Discovery Welwyn
Dr Nigel Rogers was formerly Director of Pre-clinical Science at Roche Discovery Welwyn and was instrumental in introducing new early ADMET approaches to enable better selection and design of compounds in Lead Optimisation. Nigel has also extensive experience of the process from Lead Identification through to NDA filing with responsibilities including project management, regulatory affairs and leadership of several projects.
Dr Will Watson
Scientific Update
Will Watson gained his PhD in Organic Chemistry from the University of Leeds in 1980. He joined the BP Research Centre at Sunbury-on-Thames and spent five and a half years working as a research chemist on a variety of topics including catalytic dewaxing, residue upgrading, synthesis of novel oxygenates for use as gasoline supplements, surfactants for use as gasoline detergent additives and non-linear optical compounds. ...
Course programme
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 Overview:
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 ligandbased 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, participants 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 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.
Medicinal Chemistry