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3,5-二苯基-1H-吡唑衍生物。II-N-取代的1-(2-氨基乙基)-3,5-二苯基-1H-吡唑及其具有镇痛和其他活性的4-溴衍生物。

3,5-Diphenyl-1H-pyrazole derivatives. II--N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives with analgesic and other activities.

作者信息

Bondavalli F, Bruno O, Ranise A, Schenone P, Russo S, Loffreda A, De Novellis V, Lo Sasso C, Marmo E

机构信息

Istituto di Scienze Farmaceutiche, Università di Genova, Italy.

出版信息

Farmaco Sci. 1988 Dec;43(12):1019-34.

PMID:3248592
Abstract

The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.

摘要

描述了通过伯胺和仲胺与1-(2-羟乙基)-3,5-二苯基-1H-吡唑及其4-溴衍生物的对甲苯磺酸酯反应合成N-取代的1-(2-氨基乙基)-3,5-二苯基-1H-吡唑及其4-溴衍生物(V)。一些化合物(V)在小鼠中表现出显著的镇痛活性。此外,上述化合物在大鼠中通常表现出适度的降压、减慢心率和抗炎活性,在小鼠中表现出浸润麻醉作用,以及在体外具有较弱的血小板抗聚集活性。

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