Title of article
Design, synthesis and structure–Activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists
Author/Authors
Timothy D. Gross، نويسنده , , Yun-Fei Zhu، نويسنده , , John Saunders، نويسنده , , Keith M. Wilcoxen، نويسنده , , Yinghong Gao، نويسنده , , Patrick J. Connors Jr.، نويسنده , , Zhiqiang Guo، نويسنده , , R. Scott Struthers، نويسنده , , Greg J. Reinhart، نويسنده , , Chen Chen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
3
From page
2185
To page
2187
Abstract
SAR studies of lead GnRH receptor antagonists 2a and 2b reported earlier resulted in the discovery of compound 10b which showed much higher potency (Ki=4.6 nM, compared with 2b, Ki=230 nM) in which the 7-position of the imidazolo[1,2-a]pyrimidone core was substituted with a methyl group, and the ester at the 6-position was replaced by the 3-methoxyphenyl group.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792404
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