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3,5-二苯基-1H-吡唑衍生物。IV——具有镇静、抗血小板聚集和局部麻醉活性的N,N-二取代3-(3,5-二苯基-1H-吡唑-1-基)丙酰胺和3-(3,5-二苯基-1H-吡唑-1-基)丙胺

3,5-Diphenyl-1H-pyrazole derivatives. IV--N,N-disubstituted 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamides and 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamines with sedative, platelet antiaggregating and local anesthetic activities.

作者信息

Bondavalli F, Bruno O, Ranise A, Schenone P, Losasso C, Donnoli D, Stella L, Marmo E

机构信息

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

出版信息

Farmaco. 1990 Feb;45(2):137-46.

PMID:2133991
Abstract

The synthesis of N,N-disubstituted 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamides 2 a-d and 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamines 3 a-d starting from 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanoic acid is described. Some of the above compounds showed considerable sedative and local anesthetic activities in mice, as well as a remarkable platelet antiaggregating activity in vitro. Moreover, the above compounds usually exhibited moderate analgesic and antiinflammatory activities in mice and rats, respectively.

摘要

描述了从3-(3,5-二苯基-1H-吡唑-1-基)丙酸出发合成N,N-二取代的3-(3,5-二苯基-1H-吡唑-1-基)丙酰胺2 a-d和3-(3,5-二苯基-1H-吡唑-1-基)丙胺3 a-d的方法。上述一些化合物在小鼠中表现出相当的镇静和局部麻醉活性,以及在体外具有显著的血小板抗聚集活性。此外,上述化合物通常在小鼠和大鼠中分别表现出适度的镇痛和抗炎活性。

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