Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

Authors
Walsh, TF Toupence, RB Young, JR Huang, SX Ujjainwalla, F DeVita, RJ Goulet, MT Wyvratt, MJ Fisher, MH Lo, JL Ren, N Yudkovitz, JB Yang, YT Cheng, K Smith, RG
Citation
Tf. Walsh et al., Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides, BIOORG MED, 10(5), 2000, pp. 443-447
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
5
Year of publication
2000
Pages
443 - 447
Database
ISI
SICI code
0960-894X(20000306)10:5<443:PAOGRH>2.0.ZU;2-Q
Abstract
SAR studies which focused upon the C-6 position of a recently described ser ies of quinolone gonadotropin releasing hormone antagonists, are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the p alladium-catalyzed amino-carbonylation reactions of iodide 4 with various a mines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier science Ltd. All rights reserved.