Bruno O, Ranise A, Bondavalli F, Schenone P, D'Amico M, Lampa E, Falzarano C, Rossi F
Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.
Farmaco. 1992 Oct;47(10):1235-48.
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.
描述了通过1-肼基-2-丙醇与二苯甲酰甲烷反应合成1-(2-羟丙基)-3,5-二苯基-1H-吡唑1,通过伯胺和仲胺与1的对甲苯磺酸盐反应合成N-取代的1-(2-氨基丙基)-3,5-二苯基-1H-吡唑3,以及从3,5-二苯基-1H-吡唑出发合成N-取代的1-(3-氨基-2-羟丙基)-3,5-二苯基-1H-吡唑6。一些化合物3和6在大鼠中显示出显著的抗炎活性,在小鼠和大鼠中还具有微弱的镇痛、解热、抗心律失常、降压活性,在体外具有中等的血小板抗聚集作用。