2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles with high affinity and selectivity for the dopamine D-3 receptor

被引：15

作者：

Bolton, D ^{[1
]}

Boyfield, I ^{[1
]}

Coldwell, MC ^{[1
]}

Hadley, MS ^{[1
]}

Johns, A ^{[1
]}

Johnson, CN ^{[1
]}

Markwell, RE ^{[1
]}

Nash, DJ ^{[1
]}

Riley, GJ ^{[1
]}

Scott, EE ^{[1
]}

Smith, SA ^{[1
]}

Stemp, G ^{[1
]}

Wadsworth, HJ ^{[1
]}

Watts, EA ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(97)00045-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles (8 - 15) has been prepared to investigate the effect on affinity and selectivity for the dopamine Dg receptor of modifying the substituent in the phenyl ring at the 2-position of the pyrrole. Sulfonate 7 and sulfonamides 12, 14, 15 were shown to have high affinities (pKi's 8.0 - 8.7) and selectivities (100 - 150-fold) for the D-3 over the D-2 receptor. (C) 1997, Elsevier Science Ltd.

引用

页码：485 / 488

页数：4

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