Abstract:
:(+)- and (-)-Lesinurad were isolated as atropisomers from racemic lesinurad for the first time. No interconversion was observed between the two atropisomers under various conditions tested. The two atropisomers showed significant differences in hURAT1 highly expressed HEK293 cell-based inhibition assays, monkey pharmacokinetic studies, and in vitro human recombinant CYP2C9 stability studies. It was speculated that (+)-lesinurad might offer a better hyperuricemia/gout therapy than (-)-lesinurad or the racemate.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Wang J,Zeng W,Li S,Shen L,Gu Z,Zhang Y,Li J,Chen S,Jia Xdoi
10.1021/acsmedchemlett.6b00465subject
Has Abstractpub_date
2017-02-14 00:00:00pages
299-303issue
3issn
1948-5875journal_volume
8pub_type
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