Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles |
| |
| Authors: | Chu L Hutchins J E Weber A E Lo J L Yang Y T Cheng K Smith R G Fisher M H Wyvratt M J Goulet M T |
| |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. lin_chu@merck.com |
| |
| Abstract: | 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. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
