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3,5-二苯基-1H-吡唑衍生物。V——具有抗心律失常、镇静和血小板抗聚集活性的1-乙酰基-4-羟基-3,5-二苯基-2-吡唑啉酯、4-羟基-3,5-二苯基-1H-吡唑酯以及N-取代的4-(3-氨基-2-羟基-1-丙氧基)-1-甲基-3,5-二苯基-1H-吡唑

3,5-Diphenyl-1H-pyrazole derivatives. V--1-Acetyl-4-hydroxy-3,5-diphenyl-2-pyrazoline esters, 4-hydroxy-3,5-diphenyl-1H-pyrazole esters and N-substituted 4-(3-amino-2-hydroxy-1-propoxy)-1-methyl-3,5-diphenyl-1H-pyrazoles with antiarrhythmic, sedative and platelet antiaggregating activities.

作者信息

Bruno O, Bondavalli F, Ranise A, Schenone P, Losasso C, Cilenti L, Matera C, Marmo E

机构信息

Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.

出版信息

Farmaco. 1990 Feb;45(2):147-66.

PMID:2133992
Abstract

The synthesis of 1-acetyl-4-hydroxy-3,5-diphenyl-2-pyrazoline esters 3, 4-hydroxy-3,5-diphenyl-1H-pyrazole esters 5 and N-substituted 4-(3-amino-2-hydroxy-1-propoxy)-1-methyl-3,5-diphenyl-1H-pyrazoles 7, starting from 4-hydroxy-3,5-diphenyl-2-pyrazoline is described. Some of compounds 3, 5 and 7 showed a considerable antiarrhythmic and sedative activity in rats and mice, respectively, as well as a remarkable in vitro platelet antiaggregating activity. Moreover, the above compounds usually exhibited moderate antihypertensive, local anesthetic, analgesic and antiinflammatory activities in rats and mice.

摘要

描述了从4-羟基-3,5-二苯基-2-吡唑啉出发合成1-乙酰基-4-羟基-3,5-二苯基-2-吡唑啉酯3、4-羟基-3,5-二苯基-1H-吡唑酯5和N-取代的4-(3-氨基-2-羟基-1-丙氧基)-1-甲基-3,5-二苯基-1H-吡唑7。化合物3、5和7中的一些分别在大鼠和小鼠中显示出相当的抗心律失常和镇静活性,以及显著的体外血小板抗聚集活性。此外,上述化合物通常在大鼠和小鼠中表现出适度的降压、局部麻醉、镇痛和抗炎活性。

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