Optimising inhibitors of trypanothione reductase using solid-phase chemistry


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

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Description/Abstract

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.

Item Type: Article
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Keywords: trypanosoma-cruzi, target, design, potent, drugs
Subjects: Q Science
Q Science > QD Chemistry
Divisions: University Structure - Pre August 2011 > School of Chemistry
ePrint ID: 18942
Date Deposited: 19 Jan 2006
Last Modified: 27 Mar 2014 18:08
URI: http://eprints.soton.ac.uk/id/eprint/18942

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