Author/Authors :
Lin Chu، نويسنده , , Jennifer E. Hutchins، نويسنده , , Ann E. Weber، نويسنده , , Jane-Ling Lo، نويسنده , , Yi-Tien Yang، نويسنده , , Kang Cheng، نويسنده , , Roy G. Smith، نويسنده , , Michael H. Fisher، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Mark T. Goulet، نويسنده ,
Abstract :
A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.
