New 4-(4-methyl-phenyl)phthalazin-1(2H)-one derivatives and their effects on α1-receptors

被引：22

作者：

Strappaghetti, G

Brodi, C

Giannaccini, G

Betti, L

机构：

[1] Univ Perugia, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy

[2] Univ Pisa, Dipartimento Psichiatria Neurobiol Farmacol & Bio, I-56126 Pisa, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

alpha(1)-adrenoceptor affinity; alpha(2)-adrenoceptor affinity; 5HT(1A)-serotoninergic affinity; phenyl-phthalazinone fragment; arylpiperazines; structure-activity relationships (SAR);

D O I：

10.1016/j.bmcl.2006.02.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Continuing our research aimed at obtaining new Compounds with high affinity and selectivity toward alpha(1)-AR, a new series of arylpiperazine derivatives was designed, synthesized, and biologically tested. The new Compounds 1-17 are characterized by a phenylphthalazin-1(2H)-one fragment connected through an alkyl chain to an arylpiperazine residue. The pharmacological profile of these compounds was evaluated for their affinity and selectivity toward alpha(1)-AR, alpha(2)-AR and toward 5HT(1A) serotoninergic receptor. A discussion on the structure-activity relationship (SAR) of these compounds is also reported. (C) 2006 Published by Elsevier Ltd.

引用

页码：2575 / 2579

页数：5

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