Benzofuranyl 3,5-bis-polyamine derivatives as time-dependent inhibitors of trypanothione reductase

Hamilton, C. J., Saravanamuthu, A., Fairlamb, A. H. and Eggleston, I. M. (2003) Benzofuranyl 3,5-bis-polyamine derivatives as time-dependent inhibitors of trypanothione reductase. Bioorganic & Medicinal Chemistry, 11 (17). pp. 3683-3693. ISSN 0968-0896

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Abstract

The synthesis and evaluation of 3,5-disubstituted benzofuran derivatives as time-dependent inhibitors of the protozoan oxidoreductase trypanothione reductase are reported. These molecules were designed as simplified mimetics of the naturally occurring spermidine-bridged macrocyclic alkaloid lunarine 1, a known time-dependent inhibitor of trypanothione reductase. In this series of compounds the bis-polyaminoacrylamide derivatives 2-4 were all shown to be competitive inhibitors, but only the bis-4-methyl-piperazin-1-yl-propylacrylamide derivative 4 displayed time-dependent activity. The kinetics of time dependent inactivation of trypanothione reductase by 1 and 4 have been determined and are compared and discussed herein. (C) 2003 Elsevier Ltd. All rights reserved.

Item Type: Article
Uncontrolled Keywords: erythrocytes,oxidative stress,glutathione-reductase
Faculty \ School: Faculty of Science > School of Pharmacy
Depositing User: Rachel Smith
Date Deposited: 18 May 2011 09:44
Last Modified: 31 Oct 2019 14:02
URI: https://ueaeprints.uea.ac.uk/id/eprint/30700
DOI: 10.1016/s0968-0896(03)00344-4

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