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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Official URL: http://dx.doi.org/10.1016/S0960-894X(00)00471-6
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 |
|---|---|
| Uncontrolled Keywords: | trypanosoma-cruzi, target, design, potent, drugs |
| Related URLs: | http://dx.doi.org/10.1016/S096...00)00471-6 |
| Subjects: | Q Science Q Science > QD Chemistry |
| Divisions: | University Structure - Pre August 2011 > School of Chemistry |
| ePrint ID: | 18942 |
| URI: | http://eprints.soton.ac.uk/id/eprint/18942 |
| Deposited On: | 19 Jan 2006 |
| Last Modified: | 01 Jun 2011 14:35 |
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