Author/Authors :
Richard A. Hartz، نويسنده , , Argyrios G. Arvanitis، نويسنده , , Charles Arnold، نويسنده , , Joseph P. Rescinito، نويسنده , , Kimberly L. Hung، نويسنده , , Ge Zhang، نويسنده , , Harvey Wong، نويسنده , , David R. Langley، نويسنده , , Paul J. Gilligan، نويسنده , , George L. Trainor، نويسنده ,
Abstract :
A novel series of 2-anilino-3-phenylsulfonyl-6-methylpyridines was synthesized and evaluated as corticotropin-releasing factor receptor ligands. Structure–activity relationship studies focused primarily on optimization of the 3-phenylsulfonyl group. Compounds within this series were identified which showed potent binding affinity for the CRF1 receptor. Selected compounds were examined in a rat pharmacokinetic study and were found to have oral bioavailabilities ranging from 16 to 35%.
