265324-40-1Relevant articles and documents
Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides
Walsh, Thomas F.,Toupence, Richard B.,Young, Jonathan R.,Huang, Song X.,Ujjainwalla, Feroze,Devita, Robert J.,Goulet, Mark T.,Wyvratt Jr., Matthew J.,Fisher, Michael H.,Lo, Jane-Ling,Ren, Ning,Yudkovitz, Joel B.,Yang, Yi Tien,Cheng, Kang,Smith, Roy G.
, p. 443 - 447 (2000)
SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.