Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus

Authors
Ashton, WT Sisco, RM Yang, YT Lo, JL Yudkovitz, JB Gibbons, PH Mount, GR Ren, RN Butler, BS Cheng, K Goulet, MT
Citation
Wt. Ashton et al., Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus, BIOORG MED, 11(13), 2001, pp. 1727-1731
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
13
Year of publication
2001
Pages
1727 - 1731
Database
ISI
SICI code
0960-894X(20010709)11:13<1727:PNGRAD>2.0.ZU;2-T
Abstract
A pyridine side-chain terminus has been incorporated into the indole-5-carb oxamide and indole-5-acetamide series of GnRH antagonists. Potent activity was observed in binding and functional assays. Certain branched or cyclic t ertiary amides were identified as preferred in each series. Alkylation of t he side-chain secondary amine had generally unfavorable effects. Variations of the gem-dialkyl substituents in the indole-5-acetamide series were also investigated. (C) 2001 Elsevier Science Ltd. All rights reserved.