Substituted indole-5-carboxamides and-acetamides as potent nonpeptide GnRH receptor antagonists

…, JL Lo, JB Yudkovitz, K Cheng, MT Goulet

Index: Ashton, Wallace T.; Sisco, Rosemary M.; Yang, Yi Tien; Lo, Jane-Ling; Yudkovitz, Joel B.; Cheng, Kang; Goulet, Mark T. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 13 p. 1723 - 1726

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Citation Number: 48

Abstract

The 2-aryltryptamine class of GnRH receptor antagonists has been modified to incorporate carboxamide and acetamide substituents at the indole 5-position. With either a phenol or methanesulfonamide terminus on the N-aralkyl side chain, potent binding affinity to the GnRH receptor was achieved. A functional assay for GnRH antagonism was even more sensitive to structural modification and revealed a strong preference for branched tertiary ...