4,5-functionalized 6-phenyl-3(2H)-pyridazinones: Synthesis and evaluation of antinociceptive activity

被引：56

作者：

DalPiaz, V

Giovannoni, MP

Ciciani, G

Barlocco, D

Giardina, G

Petrone, G

Clarke, GD

机构：

[1] UNIV MODENA,DIPARTIMENTO SCI FARMACEUT,I-41100 MODENA,ITALY

[2] SMITHKLINE BEECHAM PHARMACEUT,I-20021 MILAN,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 31卷 / 01期

关键词：

Emorfazone; pyridazinone; antinociceptive activity;

D O I：

10.1016/S0223-5234(96)80008-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-substituted 4,5-functionalized 6-phenyl-3(2H)-pyridazinones were synthesized and their antinociceptive activities were evaluated in the mouse abdominal constriction model. Single dose studies showed that compounds 11, 18a and 23 were more active than the reference drug, Emorfazone, in inhibiting the effects of the noxious chemical stimulus, p-phenylquinone. Subsequent dose-response studies revealed 18a to be almost seven-fold more potent than Emorfazone.

引用

页码：65 / 70

页数：6

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