Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant ROR?t Inhibitors.

ABSTRACT: A novel series of biaryl amides was identified as ROR?t inhibitors through core replacement of a starting hit 1. Structure-activity relationship exploration on the biaryl moiety led to discovery of potent ROR?t inhibitors with good oral bioavailability and CNS penetration. Compounds 9a and 9g demonstrated excellent in vivo efficacy in EAE mice dose dependently with once daily oral administration.

SUBMITTER: Wang Y 

PROVIDER: S-EPMC4499822 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature