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Details of Grant 

EPSRC Reference: GR/L02210/01
Title: SYNTHESIS OF NOVEL AMINO ACIDS AS GLUTAMATE RECEPTOR LIGANDS AND NO SYNTHASE INHIBITORS
Principal Investigator: Young, Professor D
Other Investigators:
Researcher Co-Investigators:
Project Partners:
GlaxoSmithKline plc (GSK) Pre Nexus Migration
Department: Chemistry
Organisation: University of Sussex
Scheme: LINK
Starts: 01 October 1996 Ends: 31 March 2000 Value (£): 36,230
EPSRC Research Topic Classifications:
Asymmetric Chemistry
EPSRC Industrial Sector Classifications:
Pharmaceuticals and Biotechnology
Related Grants:
Panel History:  
Summary on Grant Application Form
N-protected pyroglutamic esters will be investigated as chiral templates for the synthesis of compounds which are specifically designed for their activity in several major therapeutic areas. The application of solid phase methodology to the chemistry will be studied and the method applied to combinatorial synthesis. Approaches to asymmetric synthesis using the pyroglutamate template will include alkylation and aldol reactions, including use of aldehydes which already contain one or more chiral centres. 4-Exo-alkylidene compounds will be prepared and 1,3-dipolar addition and Diels Alder reactions, epoxidation and aziridination will be investigated. Nucleophilic attack on the epoxides and aziridines will allow the creation of compounds containing two new chiral centres in addition to that already present. Ring opening to acyclic synthons which can be further elaborated or ring switching methodology will allow us to gain access to target compounds which will be agonists or antagonists at glutamate binding sites or to cyclic analogues of arginine as possible NO synthase inhibitors.
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Organisation Website: http://www.sussex.ac.uk