A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes

A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes

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)­sulf...

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Veröffentlicht in:Journal of medicinal chemistry 2014-02, Vol.57 (4), p.1616-1620
Hauptverfasser: O’Hara, Fionn, Burns, Aaron C, Collins, Michael R, Dalvie, Deepak, Ornelas, Martha A, Vaz, Alfin D. N, Fujiwara, Yuta, Baran, Phil S
Format: Artikel
Sprache:eng
Schlagworte:
Aldehyde Oxidase - metabolism
Brief
Hydrocarbons - metabolism
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Zusammenfassung: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm4017976