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

被引:9
作者
Boyfield, I [1 ]
Coldwell, MC [1 ]
Hadley, MS [1 ]
Healy, MAM [1 ]
Johnson, CN [1 ]
Nash, DJ [1 ]
Riley, GJ [1 ]
Scott, EE [1 ]
Smith, SA [1 ]
Stemp, G [1 ]
机构
[1] SMITHKLINE BEECHAM PHARMACEUT, HARLOW CM19 5AW, ESSEX, ENGLAND
关键词
D O I
10.1016/S0960-894X(96)00621-X
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 (4-26) has been prepared where the conformational requirements of the N-ethyl, N-benzyl side-chain of 1 and the effect of introducing substituents into the benzyl group have been investigated. The (R)-alpha-methylbenzyl 6 and aminoindane 10 side-chains retained high affinity for the dopamine Dg receptor, although neither showed the selectivity of 2-phenylazacycloheptane 2. (C) 1997, Elsevier Science Ltd.
引用
收藏
页码:327 / 330
页数:4
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