A simple litmus test for aldehyde oxidase metabolism of heteroarenes.
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ABSTRACT:
SUBMITTER: O'Hara F
PROVIDER: S-EPMC3983350 | biostudies-literature | 2014 Feb
REPOSITORIES: biostudies-literature
Publications
A simple litmus test for aldehyde oxidase metabolism of heteroarenes.
O'Hara Fionn F Burns Aaron C AC Collins Michael R MR Dalvie Deepak D Ornelas Martha A MA Vaz Alfin D N AD Fujiwara Yuta Y Baran Phil S PS
Journal of medicinal chemistry 20140205 4
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 metabol ...[more]
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