Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor

被引：29

作者：

Baraldi, PG ^{[1
]}

Romagnoli, R

Tabrizi, MA

Falzoni, S

Di Virgilio, F

机构：

[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[2] Univ Ferrara, Sez Patol Gen, Dipartimento Med Diagnost & Sperimentale, I-44100 Ferrara, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(00)00083-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Conformationally constrained analogues of KN62 containing 1,2,3,4-tetrahydro-7-hydroxyisoquinoline-3-carboxylic acid with S configuration in position 3 were synthesized and their antagonist activities were tested on human macrophage cells. While KN62 is a potent antagonist of the P2X(7) receptor, these analogues were inactive as antagonists and only one compound showed appreciable activity as P2X(7) antagonist, which was 30 times weaker than that reported for KN62. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：681 / 684

页数：4

共 25 条

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