Bondavalli F, Bruno O, Ranise A, Schenone P, Losasso C, Stella L, de Paola C, Ioia N, Marmo E
Istituto di Scienze Farmaceutiche dell'Università Viale Benedetto XV, Genova, Italy.
Farmaco. 1990 May;45(5):511-26.
The syntheses of 1-(2-hydroxy-2-phenylethyl)-3,5-diphenyl-1H-pyrazole 1 by reaction of 2-hydrazino-1-phenylethanol with dibenzoylmethane, of esters 2 and 2-dialkylaminoethyl ethers 3 starting from 1 as sodium salt and acyl chlorides or 2-chloroethyldialkylamines, respectively, as well as of N,N-disubstituted 1-(2-amino-2-phenylethyl)-3,5-diphenyl-1H-pyrazoles 5 by reaction of secondary amines with the tosylate of 1, are described. Some of the above compounds showed a considerable sedative effect in mice and a remarkable platelet antiaggregating activity in vitro, as well as moderate local anesthetic, analgesic and antiinflammatory activities in mice and rats.
描述了通过2-肼基-1-苯乙醇与二苯甲酰甲烷反应合成1-(2-羟基-2-苯乙基)-3,5-二苯基-1H-吡唑1，从1的钠盐分别与酰氯或2-氯乙基二烷基胺出发合成酯2和2-二烷基氨基乙基醚3，以及通过仲胺与1的对甲苯磺酸盐反应合成N,N-二取代的1-(2-氨基-2-苯乙基)-3,5-二苯基-1H-吡唑5。上述一些化合物在小鼠中显示出相当大的镇静作用，在体外具有显著的血小板抗聚集活性，以及在小鼠和大鼠中具有适度的局部麻醉、镇痛和抗炎活性。
