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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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.
|Digital Object Identifier (DOI):||doi:10.1016/S0960-894X(00)00471-6|
|Keywords:||trypanosoma-cruzi, target, design, potent, drugs|
Q Science > QD Chemistry
|Divisions:||University Structure - Pre August 2011 > School of Chemistry
|Date Deposited:||19 Jan 2006|
|Last Modified:||31 Mar 2016 11:35|
|RDF:||RDF+N-Triples, RDF+N3, RDF+XML, Browse.|
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