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A simple litmus test for aldehyde oxidase metabolism of heteroarenes.

Abstract：

: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 "litmus test" for the early identification of heteroaromatic drug candidates that have a high probability of metabolism by AO.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

O'Hara F,Burns AC,Collins MR,Dalvie D,Ornelas MA,Vaz AD,Fujiwara Y,Baran PS

doi

10.1021/jm4017976

subject

Has Abstract

pub_date

2014-02-27 00:00:00

pages

1616-20

issue

4

eissn

0022-2623

issn

1520-4804

journal_volume

57

pub_type

杂志文章

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