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.
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页码：171 / 190
页数：20
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