Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents

被引：211

作者：

Chibale, K ^{[1
]}

Visser, M

van Schalkwyk, D

Smith, PJ

Saravanamuthu, A

Fairlamb, AH

机构：

[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa

[2] Univ Dundee, Wellcome Trust Bioctr, Sch Life Sci, Div Biol Chem & Mol Microbiol, Dundee DD1 5EH, Scotland

[3] Univ Cape Town, Sch Med, Dept Med, Div Pharmacol, ZA-7925 Cape Town, South Africa

来源：

TETRAHEDRON | 2003年 / 59卷 / 13期

基金：

英国惠康基金; 新加坡国家研究基金会;

关键词：

9,9-dimethylxanthenes; trypanothione reductase inhibitors; chloroquine potentiating agents; trypanosomiasis; leishmaniasis; malaria;

D O I：

10.1016/S0040-4020(03)00240-0

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学]; 081704 [应用化学];

摘要：

Xanthene derivatives were synthesized and evaluated for their potential as trypanothione reductase (TryR) inhibitors and chloroquine (CQ) potentiating agents. Some derivatives displayed inhibitory activity against TryR comparable to known tricyclic antidepressants. On the other hand a number of derivatives increased CQ accumulation and potentiating effects in a resistant strain of Plasmodium falciparum with one compound also displaying strong intrinsic antimalarial activity. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：2289 / 2296

页数：8

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