Author/Authors :
Robert J. DeVita، نويسنده , , Darius D. Hollings، نويسنده , , Mark T. Goulet، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Michael H. Fisher، نويسنده , , Jane-L. Lo، نويسنده , , Yi Tien Yang، نويسنده , , Kang Cheng، نويسنده , , Roy G. Smith، نويسنده ,
Abstract :
Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (−300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chloro-substitution of the 1H-quinolone core.
