SYNTHESIS AND TRAZODONE-LIKE PHARMACOLOGICAL PROFILE OF 1- AND 2-[3-[4-(X)-1-PIPERAZINYL]-PROPYL]BENZOTRIAZOLES

被引：38

作者：

CALIENDO, G

DICARLO, R

MELI, R

PERISSUTTI, E

SANTAGADA, V

SILIPO, C

VITTORIA, A

机构：

[1] UNIV FEDERICO II,DIPARTIMENTO FARMACOL SPERIMENTALE,I-80131 NAPLES,ITALY

[2] UNIV FEDERICO 11,DIPARTIMENTO CHIM FARMACEUT & TOSSICOL,VIA D MONTESANO 49,I-80131 NAPLES,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 28卷 / 12期

关键词：

BENZOTRIAZOLES; ANTISEROTONERGIC; ANTIADRENERGIC; ANTIHISTAMINIC; ANALGESIC;

D O I：

10.1016/0223-5234(93)90053-H

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1- and 2-[3-[4-(X)-1-piperazinyl]-propyl]benzotriazoles were prepared and evaluated for their trazodone like pharmacological profile; as preliminary pharmacological screening, the compounds were tested for their antiserotonergic, antiadrenergic and antihistaminic in vitro activity as well as for their analgesic in vivo action. Structure-activity relationships showed that among the synthesized compounds, the analogues bearing on the 4-piperazine nitrogen either an unsubstituted phenyl ring or a 2- or 3-chloro phenyl moiety show a pharmacological profile similar to that of the antidepressant trazodone.

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页码：969 / 974

页数：6

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