3,5-DIPHENYL-1H-PYRAZOLE DERIVATIVES .9. 2-SUBSTITUTED 4-PHENYL-5-(3,5-DIPHENYL-1H-PYRAZOL-1-YL) PYRIMIDINES WITH PLATELET ANTIAGGREGATING AND OTHER ACTIVITIES

被引：0

作者：

BONDAVALLI, F ^{[1
]}

BRUNO, O ^{[1
]}

RANISE, A ^{[1
]}

SCHENONE, P ^{[1
]}

DAMICO, M ^{[1
]}

PARRILLO, C ^{[1
]}

FILIPPELLI, W ^{[1
]}

ROSSI, F ^{[1
]}

机构：

[1] UNIV FEDERICO II,FAC MED & CHIRURG 1,IST FARMACOL & TOSSICOL,I-80138 NAPLES,ITALY

来源：

FARMACO | 1992年 / 47卷 / 02期

关键词：

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The synthesis of 2-substituted 4-phenyl-5-(3,5-diphenyl-1H-pyrazol-1-yl)pyrimidines 4 a-e by reaction of 1-(1-dimethylaminomethylene-2-oxo-2-phenylethyl)-3,5-diphenyl-1H-pyrazole with acetamidine, benzamidine, guanidine, guanidineacetic acid and creatine, respectively, is described. The alpha-aminoacid derivatives 4 d and 4 e gave a series of amides 7 by coupling with primary or secondary amines in dimethylformamide (DMF) solution in the presence of diphenyl-phosphorylazide (DPPA) and triethylamine. Some compounds 4 and 7 showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as moderate antihypertensive, local anesthetic, analgesic and antiinflammatory activities in rats and mice.

引用

页码：171 / 190

页数：20

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