High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity
High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity
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DOI：
10.1016/j.bmcl.2006.12.016
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发表时间：
2007-03-01
影响因子：
2.7
通讯作者：
Clardy, Jon
中科院分区：
文献类型：
--
作者：
Martyn, Derek C.;Jones, Deuan C.;Clardy, Jon
针对含有约134，500种化合物的商业库筛选了锥虫硫酮还原酶（TR），这是一种缓冲锥虫寄生虫氧化应激的酶。二次筛选后，四种化学型被鉴定为筛选阳性，对TR的选择性超过人谷胱甘肽还原酶。从这四个chernotypes购买了13个化合物，并描述了它们对TR和布氏锥虫的体外活性。(c)2006爱思唯尔有限公司保留所有权利。
Trypanothione reductase (TR), an enzyme that buffers oxidative stress in trypanosomatid parasites, was screened against commercial libraries containing approximately 134,500 compounds. After secondary screening, four chemotypes were identified as screening positives with selectivity for TR over human glutathione reductase. Thirteen compounds from these four chernotypes were purchased, and their in vitro activity against TR and Trypanosoma brucei is described. (c) 2006 Elsevier Ltd. All rights reserved.