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3,5-二苯基-1H-吡唑衍生物。XI. N-芳基-5(3)-苯基-4-(3,5-二苯基-1-吡唑基)-3(5)-吡唑胺、5-取代的4,5-二氢-3-苯基-4-(3,5-二苯基-1-吡唑基)-1H-吡唑以及具有解热、抗炎和其他活性的2,6-二取代-1,6-二氢-4-苯基-5-(3,5-二苯基-1-吡唑基)嘧啶

3,5-diphenyl-1H-pyrazole derivatives. XI. N-aryl-5(3)-phenyl-4-(3,5- diphenyl-1-pyrazolyl)-3(5)-pyrazole amines, 5-substituted 4,5-dihydro-3-phenyl-4-(3,5-diphenyl-1-pyrazolyl)-1H-pyrazoles and 2,6-disubstituted 1,6-dihydro-4- phenyl-5-(3,5-diphenyl-1-pyrazolyl)pyrimidines with antipyretic, antiinflammatory and other activities.

作者信息

Bruno O, Ranise A, Bondavalli F, Schenone P, D'Amico M, Filippelli A, Filippelli W, Rossi F

机构信息

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

出版信息

Farmaco. 1993 Jul;48(7):949-66.

PMID:8397678
Abstract

The synthesis of N-aryl-5(3)-phenyl-4-(3,5-diphenyl-1-pyrazolyl)-3(5)- pyrazoleamines 3 by reaction of some N-aryl-3-oxo-3-phenyl-2-(3,5-diphenyl-1- pyrazolyl)propanecarbothioamides with hydrazine is described. Also prepared were 4,5-dihydro-3-phenyl-4-(3,5-diphenyl-1-pyrazolyl)-1H-pyrazoles 6 and 1,6-dihydro-4-phenyl-5-(3,5-diphenyl-1-pyrazolyl)pyrimidines 7 by reaction of 1-phenyl-2-(3,5-diphenyl-1-pyrazolyl)-2-buten-1-one with hydrazine or guanidine and benzamidine, respectively. Some compounds 3, 6 and 7 showed remarkable antipyretic, antiinflammatory and in vitro platelet antiaggregating activities, as well as weak analgesic, antiarrhythmic, hypotensive and local anesthetic activities in rats and mice.

摘要

描述了一些N-芳基-3-氧代-3-苯基-2-(3,5-二苯基-1-吡唑基)丙烷硫代酰胺与肼反应合成N-芳基-5(3)-苯基-4-(3,5-二苯基-1-吡唑基)-3(5)-吡唑胺3的过程。还分别通过1-苯基-2-(3,5-二苯基-1-吡唑基)-2-丁烯-1-酮与肼或胍和苯甲脒反应制备了4,5-二氢-3-苯基-4-(3,5-二苯基-1-吡唑基)-1H-吡唑6和1,6-二氢-4-苯基-5-(3,5-二苯基-1-吡唑基)嘧啶7。一些化合物3、6和7在大鼠和小鼠中表现出显著的解热、抗炎和体外血小板抗聚集活性,以及微弱的镇痛、抗心律失常、降压和局部麻醉活性。

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