A simple in vitro assay for assessing the reactivity of nitrile containing compounds

被引：56

作者：

MacFaul, Philip A. ^{[1
]}

Morley, Andrew D. ^{[1
]}

Crawford, James J. ^{[1
]}

机构：

[1] AstraZeneca, Mereside, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 04期

关键词：

Nitriles; Glutathione; Cysteine; Benchmarking; GLUTATHIONE TRANSFERASES; CATHEPSIN-K; METABOLIC-ACTIVATION; CATALYTIC MECHANISM; AQUEOUS-SOLUTIONS; THIOLS; INHIBITORS; CYSTEINE; POTENT;

D O I：

10.1016/j.bmcl.2008.12.105

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A quantitative assay involving the reaction of nitriles with glutathione and cysteine has been used as a simple in vitro screen to assess potential toxicity risk of candidate compounds in drug discovery. Studies have indicated that, when benchmarked with selected compounds, the reaction of the nitriles with glutathione can provide a useful tool for deciding whether or not to progress compounds in the absence of radiolabelling studies. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1136 / 1138

页数：3