GnRh Backup?
J Med Chem 2003 Apr 24;46(9):1769-72 Related Articles, Links
Design and Structure-Activity Relationships of 2-Alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as Potent GnRH Receptor Antagonists.
Zhu YF, Guo Z, Gross TD, Gao Y, Connors PJ Jr, Struthers RS, Xie Q, Tucci FC, Reinhart GJ, Wu D, Saunders J, Chen C.
Department of Medicinal Chemistry and Department of Exploratory Discovery, Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, California 92121.
SAR studies of 7-phenylpyrrolo[1,2-a]pyrimid-4-ones 1 and 2, and 2-phenylimidazolo[1,2-a]pyrimidines 3 and 4, as nonpeptide human GnRH receptor antagonists, lead us to believe that the aromatic ring at position-2 of 4 is no longer crucial for the binding once an aryl group is incorporated at postion-6. We report here the use of a 2-alkyl group on the imidazolo[1,2-a]pyrimidone core to generate potent GnRH receptor antagonists. This discovery enabled us to obtain smaller but equally potent GnRH receptor antagonists.
PMID: 12699396 [PubMed - in process] |
