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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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
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author O’Hara, Fionn
Burns, Aaron C.
Collins, Michael R.
Dalvie, Deepak
Ornelas, Martha A.
Vaz, Alfin D. N.
Fujiwara, Yuta
Baran, Phil S.
author_facet O’Hara, Fionn
Burns, Aaron C.
Collins, Michael R.
Dalvie, Deepak
Ornelas, Martha A.
Vaz, Alfin D. N.
Fujiwara, Yuta
Baran, Phil S.
author_sort O’Hara, Fionn
collection PubMed
description [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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spelling pubmed-39833502015-01-28 A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes O’Hara, Fionn Burns, Aaron C. Collins, Michael R. Dalvie, Deepak Ornelas, Martha A. Vaz, Alfin D. N. Fujiwara, Yuta Baran, Phil S. J Med Chem [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. American Chemical Society 2014-01-28 2014-02-27 /pmc/articles/PMC3983350/ /pubmed/24472070 http://dx.doi.org/10.1021/jm4017976 Text en Copyright © 2014 American Chemical Society
spellingShingle O’Hara, Fionn
Burns, Aaron C.
Collins, Michael R.
Dalvie, Deepak
Ornelas, Martha A.
Vaz, Alfin D. N.
Fujiwara, Yuta
Baran, Phil S.
A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
title A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
title_full A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
title_fullStr A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
title_full_unstemmed A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
title_short A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
title_sort simple litmus test for aldehyde oxidase metabolism of heteroarenes
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3983350/
https://www.ncbi.nlm.nih.gov/pubmed/24472070
http://dx.doi.org/10.1021/jm4017976
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