Mandal, Mihirbaran published the artcileOvercoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety, Application In Synthesis of 871332-95-5, the publication is Journal of Medicinal Chemistry (2018), 61(23), 10700-10708, database is CAplus and MEDLINE.
Herein the authors describe structure-activity relationship (SAR) and metabolite identification (Met-ID) studies that provided insight into the origin of time-dependent inhibition (TDI) of cytochrome P 450 3A4 (CYP3A4) by compound I. Collectively, these efforts revealed that bioactivation of the fluoropyrimidine moiety of I led to reactive metabolite formation via oxidative defluorination and was responsible for the observed TDI. The authors discovered that substitution at both the 4- and 6-positions of the 5-fluoropyrimidine of I was necessary to ameliorate this TDI as exemplified by compound II.
Journal of Medicinal Chemistry published new progress about 871332-95-5. 871332-95-5 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (4-Chloro-3-cyanophenyl)boronic acid, and the molecular formula is C7H5BClNO2, Application In Synthesis of 871332-95-5.
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