Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists

JP Simeone, RL Bugianesi, MM Ponpipom…

Index: Simeone, Joseph P; Bugianesi, Robert L; Ponpipom, Mitree M; Yang, Yi Tien; Lo, Jane-Ling; Yudkovitz, Joel B; Cui, Jisong; Mount, George R; Ren, Rena Ning; Creighton, Mellissa; Mao, An-Hua; Vincent, Stella H; Cheng, Kang; Goulet, Mark T Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 22 p. 3329 - 3332

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Citation Number: 18

Abstract

The synthesis of a number of indole GnRH antagonists is described. Oxidation of the pyridine ring nitrogen, combined with alkylation at the two position, led to a compound with an excellent in vitro activity profile as well as oral bioavailability in both rats and dogs. ... The synthesis and biological evaluation of a series of indole GnRH receptor antagonists are described. Several potent binders of the human GnRH receptor were discovered, including compound 44, ...