Silicon Investor (SI) -- The First Internet Community

STOCKTALK

We've detected that you're using an ad content blocking browser plug-in or feature. Ads provide a critical source of revenue to the continued operation of Silicon Investor. We ask that you disable ad blocking while on Silicon Investor in the best interests of our community. If you are not using an ad blocker but are still receiving this message, make sure your browser's tracking protection is set to the 'standard' level.

Biotech / Medical : Neurocrine Biosciences (NBIX) -- Ignore unavailable to you. Want to Upgrade?

To: mopgcw who wrote (1117)	5/13/2003 7:33:15 PM
From: keokalani'nui	Read Replies (1) \| Respond to of 1834

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]