Quinolones as gonadotropin releasing hormone (GnRH) antagonists: Simultaneous optimization of the C(3)-aryl and C(6)-substituents

Authors
Young, JR Huang, SX Chen, I Walsh, TF DeVita, RJ Wyvratt, MJ Goulet, MT Ren, N Lo, J Yang, YT Yudkovitz, JB Cheng, K Smith, RG
Citation
Jr. Young et al., Quinolones as gonadotropin releasing hormone (GnRH) antagonists: Simultaneous optimization of the C(3)-aryl and C(6)-substituents, BIOORG MED, 10(15), 2000, pp. 1723-1727
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
15
Year of publication
2000
Pages
1723 - 1727
Database
ISI
SICI code
0960-894X(20000807)10:15<1723:QAGRH(>2.0.ZU;2-X
Abstract
A series of 3-arylquinolones was prepared and evaluated for their ability t o act as gonadotropin releasing hormone (GnRH) antagonists. A variety of su bstitution patterns of the 3-aryl substituent are described. The 3,4,5-trim ethylphenyl substituent (23h) was found to he optimal. (C) 2000 Elsevier Sc ience Ltd. All rights reserved.