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Optimising inhibitors of trypanothione reductase using solid-phase chemistry

Record type: Article

A series of inhibitors of the enzyme trypanothione reductase has been identified using directed solid-phase chemistry. The compounds were based on a series of polyamine scaffolds and used the natural product kukoamine A as the lead structure. A compound with a K-i of 76 nM was identified, although somewhat surprisingly the compound appeared to be noncompetitive in nature.

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Citation

Chitkul, B. and Bradley, M. (2000) Optimising inhibitors of trypanothione reductase using solid-phase chemistry Bioorganic and Medicinal Chemistry Letters, 10, (20), pp. 2367-2369. (doi:10.1016/S0960-894X(00)00471-6).

More information

Published date: 16 October 2000
Keywords: trypanosoma-cruzi, target, design, potent, drugs

Identifiers

Local EPrints ID: 18942
URI: http://eprints.soton.ac.uk/id/eprint/18942
PURE UUID: 3e549ea7-db7d-479f-89d8-c74bea4e46bb

Catalogue record

Date deposited: 19 Jan 2006
Last modified: 17 Jul 2017 16:34

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Contributors

Author: B. Chitkul
Author: M. Bradley

University divisions

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