Author/Authors :
Thomas F. Walsh، نويسنده , , Richard B. Toupence، نويسنده , , Jonathan R. Young، نويسنده , , Song X. Huang، نويسنده , , Feroze Ujjainwalla، نويسنده , , Robert J. DeVita، نويسنده , , Mark T. Goulet، نويسنده , , Matthew J. WyvrattJr.، نويسنده , , Michael H. Fisher، نويسنده , , Jane-Ling Lo، نويسنده , , Ning Ren، نويسنده , , Joel B. Yudkovitz، نويسنده , , Yi Tien Yang، نويسنده , , Kang Cheng، نويسنده , , Roy G. Smith، نويسنده ,
Abstract :
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 Scheme 1 and Scheme 2 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors.