Modification of the Pyridine Moiety of Non-peptidyl Indole GnRH Receptor Antagonists.

Joseph P Simeone,Robert L Bugianesi,Mitree M Ponpipom,Yi Tien Yang,Jane-Ling Lo,Joel B Yudkovitz,Jisong Cui,George R Mount,Rena Ning Ren,Mellissa Creighton,An-Hua Mao,Stella H Vincent,Kang Cheng,Mark T Goulet

Bioorganic & Medicinal Chemistry Letters（2003）

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摘要

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.

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nitrogen

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