3,5-二苯基-1H-吡唑衍生物。VIII. N-取代的3-(4-羟基-3,5-二苯基-1H-吡唑-1-基)丙酰胺、丙胺及2-(4-羟基-3,5-二苯基-1H-吡唑-1-基)乙胺，具有抗血小板聚集、降压、抗心律失常及其他活性。
3,5-Diphenyl-1H-pyrazole derivatives. VIII. N-substituted 3-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)-propanamides, -propanamines and 2-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)ethanamines with platelet antiaggregating, hypotensive, antiarrhythmic and other activities.
作者信息
Bruno O, Bondavalli F, Ranise A, Schenone P, Cenicola M L, Donnoli D, Filippelli W, Losasso C, Costantino M, Marmo E
机构信息
Istituto di Scienze Farmaceutiche dell'Università Genova, Italy.
出版信息
Farmaco. 1991 Mar;46(3):477-99.
The synthesis of N,N-disubstituted 3-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)-propanamides and -propanamines, starting from 4-benzoyloxy-3,5-diphenyl-1H-pyrazole, and of N-substituted 2-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)ethanamines, starting from 4-acetoxy-1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole, is described. Some of the above compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as moderate hypotensive, antiarrhythmic, local anesthetic, sedative and antiinflammatory activities in rats and mice.
描述了从4-苯甲酰氧基-3,5-二苯基-1H-吡唑出发合成N,N-二取代的3-(4-羟基-3,5-二苯基-1H-吡唑-1-基)丙酰胺和丙胺，以及从4-乙酰氧基-1-(2-羟乙基)-3,5-二苯基-1H-吡唑出发合成N-取代的2-(4-羟基-3,5-二苯基-1H-吡唑-1-基)乙胺的方法。上述一些化合物在体外显示出优于或相当于乙酰水杨酸的血小板抗聚集活性，以及在大鼠和小鼠中表现出适度的降压、抗心律失常、局部麻醉、镇静和抗炎活性。
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