Synthesis and dopamine D2-like receptor binding affinity of substituted 5-phenyl-pyrrole-3-carboxamides

被引:31
作者
Pinna, GA
Curzu, MM
Sechi, M
Chelucci, G
Maciocco, E
机构
[1] Univ Sassari, Ist Chim Farmaceut & Tossicol, I-07100 Sassari, Italy
[2] Univ Sassari, Dipartimento Chim, I-07100 Sassari, Italy
[3] Univ Cagliari, Dipartimento Biol Sperimentale, I-09123 Cagliari, Italy
来源
FARMACO | 1999年 / 54卷 / 08期
关键词
D-2-like receptor binding; substituted; 5-phenyl-pyrrole-3-carboxamides; structure-activity relationship;
D O I
10.1016/S0014-827X(99)00061-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A series of 5-p-substituted phenyl-pyrrole-3-carboxamide derivatives was designed as hybrid analogs of the dopamine D-2-like 5-phenyl-pyrrole and heterocyclic carboxamide antipsychotics. The title compounds were synthesized and evaluated for dopamine D-2-like receptor by means of [H-3]YM-09151-2 receptor binding assay. The compound bearing a 1-ethyl-2-methyl-pyrrolidine moiety as the basic part of 5-phenyl-pyrrole-3-carboxamide derivative la together with its 2-chloro analog If were found to possess affinity in the low micromolar range. Substituted phenyl-pyrrolecarboxamides containing groups such as F, Cl, NO2, CH3, at the 4-position of the phenyl ring, gave ligands with lower D-2-like affinity. (C) 1999 Elsevier Science S.A. All rights reserved.
引用
收藏
页码:542 / 550
页数:9
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