Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C (3)-aryl and C (6)-substituents

…, MT Goulet, N Ren, J Lo, YT Yang, JB Yudkovitz…

Index: Young, Jonathan R.; Huang, Song X.; Chen, Irene; Walsh, Thomas F.; DeVita, Robert J.; Wyvratt Jr., Matthew J.; Goulet, Mark T.; Ren, Ning; Lo, Jane; Yang, Yi Tien; Yudkovitz, Joel B.; Cheng, Kang; Smith, Roy G. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 15 p. 1723 - 1727

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Citation Number: 28

Abstract

A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3, 4, 5-trimethylphenyl substituent (23h) was found to be optimal.

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