Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X(7)-receptor

Authors
Baraldi, PG Romagnoli, R Tabrizi, MA Falzoni, S Di Virgilio, F
Citation
Pg. Baraldi et al., Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X(7)-receptor, BIOORG MED, 10(7), 2000, pp. 681-684
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
7
Year of publication
2000
Pages
681 - 684
Database
ISI
SICI code
0960-894X(20000403)10:7<681:SOCCAO>2.0.ZU;2-U
Abstract
Conformationally constrained analogues of KN62 containing 1,2,3,4-tetrahydr o-7-hydroxyisoquinoline-3-carboxylic acid with S configuration in position 3 were synthesized and their antagonist activities were tested on human mac rophage cells. While KN62 is a potent antagonist of the P2X(7) receptor, th ese analogues were inactive as antagonists and only one compound showed app reciable activity as P2X(7) antagonist, which was 30 times weaker than that reported for KN62. (C) 2000 Elsevier Science Ltd. All rights reserved.