A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
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- 作者：Fionn O鈥橦ara ; Aaron C. Burns ; Michael R. Collins ; Deepak Dalvie ; Martha A. Ornelas ; Alfin D. N. Vaz ; Yuta Fujiwara ; Phil S. Baran
- 刊名：Journal of Medicinal Chemistry
- 出版年：2014
- 出版时间：February 27, 2014
- 年：2014
- 卷：57
- 期：4
- 页码：1616-1620
- 全文大小：398K
- 年卷期：v.57,no.4(February 27, 2014)
- ISSN：1520-4804
文摘
The bioavailability of aromatic azaheterocyclic drugs can be affected by the activity of aldehyde oxidase (AO). Susceptibility to AO metabolism is difficult to predict computationally and can be complicated in vivo by differences between species. Here we report the use of bis(((difluoromethyl)sulfinyl)oxy)zinc (DFMS) as a source of CF2H radical for a rapid and inexpensive chemical 鈥渓itmus test鈥?for the early identification of heteroaromatic drug candidates that have a high probability of metabolism by AO.