Synthesis and evaluation of 2-anilino-3-phenylsulfonyl-6-methylpyridines as corticotropin-releasing factor₁ receptor ligands

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• 作者：Richard A. Hartz ; Argyrios G. Arvanitis ; Charles Arnold ; Joseph P. Rescinito ; Kimberly L. Hung ; Ge Zhang ; Harvey Wong ; David R. Langley ; Paul J. Gilligan and George L. Trainor
• 关键词：Corticotropin-releasing factor ; CRF ; Phenylsulfone
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 February 2006
• 年：2006
• 卷：16
• 期：4
• 页码：934-937
• 全文大小：132 K

文摘

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 % .