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)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.
Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Fionn
F
O'Hara
Aaron C
AC
Burns
Michael R
MR
Collins
Deepak
D
Dalvie
Martha A
MA
Ornelas
Alfin D N
AD
Vaz
Yuta
Y
Fujiwara
Phil S
PS
Baran
D042931:Aldehyde Oxidase / Q000378:metabolism*; D006838:Hydrocarbons / Q000378:metabolism*
D006838:Hydrocarbons; D042931:Aldehyde Oxidase