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Design and synthesis of conformationally restrained amino acids and peptides

Objective



Combinatorial chemistry has developed as a novel approach to lead generation for new biological targets uncovered by advances in molecular biology. Libraries of small peptides have been prepared but the large number of conformations that are available to small unconstrained peptides limits the potencies of the "hits" that are found. It is proposed to design and prepare conformationally restricted amino acids for incorporation into libraries of small peptides. Any "hits" from such libraries may be expected to have higher potencies as compared to the "hits" from unconstrained libraries. There are two aspects to the research - firstly we need a system of confirmational analysis to aid the design of a range of analogues covering different areas of conformational space. The other aspect is the actual synthesis of specific conformationally restrained amino acids. The project will involve computational chemistry and synthetic chemistry within a medicinal chemistry setting, and provide a good training for either academia or industry.

Funding Scheme

RGI - Research grants (individual fellowships)

Coordinator

SmithKline Beecham Pharmaceuticals Ltd.
Address
Great West Road
TW8 9EP Brentford
United Kingdom

Participants (1)

Not available
Netherlands