A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes

[Image: see text] 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(((dif...

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Detalles Bibliográficos
Autores principales: O’Hara, Fionn, Burns, Aaron C., Collins, Michael R., Dalvie, Deepak, Ornelas, Martha A., Vaz, Alfin D. N., Fujiwara, Yuta, Baran, Phil S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3983350/
https://www.ncbi.nlm.nih.gov/pubmed/24472070
http://dx.doi.org/10.1021/jm4017976
Descripción
Sumario:[Image: see text] 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 CF(2)H 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.

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