Optimising inhibitors of trypanothione reductase using solid-phase chemistry
Optimising inhibitors of trypanothione reductase using solid-phase chemistry
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.
trypanosoma-cruzi, target, design, potent, drugs
2367-2369
Chitkul, B.
8f090116-13b1-4ccb-b596-322316652109
Bradley, M.
078a34d6-96c4-4ce1-9aa1-454d9ee0030d
16 October 2000
Chitkul, B.
8f090116-13b1-4ccb-b596-322316652109
Bradley, M.
078a34d6-96c4-4ce1-9aa1-454d9ee0030d
Chitkul, B. and Bradley, M.
(2000)
Optimising inhibitors of trypanothione reductase using solid-phase chemistry.
Bioorganic & Medicinal Chemistry Letters, 10 (20), .
(doi:10.1016/S0960-894X(00)00471-6).
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.
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Published date: 16 October 2000
Keywords:
trypanosoma-cruzi, target, design, potent, drugs
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Local EPrints ID: 18942
URI: http://eprints.soton.ac.uk/id/eprint/18942
PURE UUID: 3e549ea7-db7d-479f-89d8-c74bea4e46bb
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Date deposited: 19 Jan 2006
Last modified: 15 Mar 2024 06:09
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Author:
B. Chitkul
Author:
M. Bradley
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