Author/Authors :
Jinlong Jiang، نويسنده , , Robert J. DeVita، نويسنده , , Mark T. Goulet، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Jane-L. Lo، نويسنده , , Ning Ren، نويسنده , , Joel B. Yudkovitz، نويسنده , , Jisong Cui، نويسنده , , Yi T. Yang، نويسنده , , Kang Cheng، نويسنده , , Susan P. Rohrer، نويسنده ,
Abstract :
Syntheses and structure–activity relationships of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists are described. Some of substituents on the piperidine ring that were investigated included a fused phenyl group, a (6R)-trifluoromethyl group, (6S) and (6R)-methyl group. This study showed that GnRH binding potency was tolerated by a small group at the 6-position of the piperidine, and blocking the 6-position by a trifluoromethyl group reduced clearance rate and increased oral bioavailability.
