199941-88-3Relevant articles and documents
Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist
DeVita, Robert J.,Hollings, Darius D.,Goulet, Mark T.,Wyvratt, Matthew J.,Fisher, Michael H.,Lo, Jane-L,Yang, Yi Tien,Cheng, Kang,Smith, Roy G.
, p. 2615 - 2620 (2007/10/03)
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-chlorosubstitution of the 1H-quinolone core.