Bioorganic and Medicinal Chemistry Letters p. 509 - 513 (2001)
Update date:2022-09-26
Topics:
Chu, Lin
Hutchins, Jennifer E.
Weber, Ann E.
Lo, Jane-Ling
Yang, Yi-Tien
Cheng, Kang
Smith, Roy G.
Fisher, Michael H.
Wyvratt, Matthew J.
Goulet, Mark T.
A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.
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