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3,5-Diphenyl-1H-pyrazole derivatives. X. N-substituted 1-(2-aminopropyl)- and 1-(3-amino-2-hydroxypropyl)-3,5-diphenyl-1H-pyrazoles with antiinflammatory and other activities.
Farmaco (Societa chimica italiana : 1989) Pub Date : 1992-10-01
O Bruno 1 , A Ranise , F Bondavalli , P Schenone , M D'Amico , E Lampa , C Falzarano , F Rossi
Affiliation  

The syntheses of 1-(2-hydroxypropyl)-3,5-diphenyl-1H-pyrazole 1 by reaction of 1-hydrazino-2-propanol with dibenzoylmethane and of N-substituted 1-(2-aminopropyl)-3,5-diphenyl-1H-pyrazoles 3 by reaction of primary and secondary amines with the tosylate of 1, as well as of N-substituted 1-(3-amino-2-hydroxypropyl)-3,5-diphenyl-1H-pyrazoles 6 starting from 3,5-diphenyl-1H-pyrazole, are described. Some compounds 3 and 6 showed remarkable antiinflammatory activity in rats, as well as weak analgesic, antipyretic, antiarrhythmic, hypotensive activities in mice and rats and moderate platelet antiaggregating effects in vitro.

中文翻译:

3,5-二苯基-1H-吡唑衍生物。X.具有抗炎和其他活性的N-取代的1-(2-氨基丙基)-和1-(3-氨基-2-羟丙基)-3,5-二苯基-1H-吡唑。

1-肼基-2-丙醇与二苯甲酰基甲烷的反应和N-取代的1-(2-氨基丙基)-3,5-反应的合成1-(2-羟丙基)-3,5-二苯基-1H-吡唑1通过伯胺和仲胺与甲苯磺酸酯1以及N-取代的1-(3-氨基-2-羟丙基)-3,5-二苯基-1H-吡唑6的甲苯磺酸酯反应生成二苯基-1H-吡唑3描述了3,5-二苯基-1H-吡唑。一些化合物3和6在大鼠中显示出显着的抗炎活性,在小鼠和大鼠中显示出较弱的镇痛,解热,抗心律不齐,降压活性,并在体外具有中等的血小板抗聚集作用。
更新日期:2019-11-01
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