Novel 2,5-disubstituted-1H-pyrroles with high affinity for the dopamine D-3 receptor

被引：16

作者：

Bolton, D ^{[1
]}

Boyfield, I ^{[1
]}

Coldwell, MC ^{[1
]}

Hadley, MS ^{[1
]}

Healy, MAM ^{[1
]}

Johnson, CN ^{[1
]}

Markwell, RE ^{[1
]}

Nash, DJ ^{[1
]}

Riley, GJ ^{[1
]}

Stemp, G ^{[1
]}

Wadsworth, HJ ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT, HARLOW CM19 5AW, ESSEX, ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 11期

关键词：

D O I：

10.1016/0960-894X(96)00202-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2,5-disubstituted-1H-pyrroles (4-18) has been prepared based on replacement of the amide of sultopride 1 by a pyrrole ring. Subsequent modification of the basic side chain gave compounds with high affinity for the dopamine D-3 receptor. In addition, 12 and 17 were shown to be D-3 antagonists with 30-fold selectivity for the D-3 receptor over the D-2 receptor. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1233 / 1236

页数：4

共 6 条

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