Menozzi G, Mosti L, Schenone P, D'Amico M, Filippelli A, Rossi F
Istituto di Scienze Farmaceutiche, Universita, Genova, Italy.
Farmaco. 1992 Dec;47(12):1495-511.
The synthesis of a series of 1-aryl-1,6-dihydro-4H-thieno[3,4-c]pyrazol-4-ones by cyclization of 3-[(2-arylhydrazino)methylene]thiophene-2,4(3H,5H)-diones, prepared by reacting 3-dimethylaminomethylenethiophene-2,4(3H,5H)-dione with arylhydrazines, is described. The 4-fluorophenyl derivative showed remarkable analgesic, antiinflammatory and antipyretic activities in mice or rats, as well as a platelet antiaggregating activity in vitro comparable to that of acetylsalicylic acid.
通过使3 - 二甲基氨基亚甲基噻吩 - 2,4(3H,5H) - 二酮与芳基肼反应制备的3 - [(2 - 芳基肼基)亚甲基]噻吩 - 2,4(3H,5H) - 二酮环化，描述了一系列1 - 芳基 - 1,6 - 二氢 - 4H - 噻吩并[3,4 - c]吡唑 - 4 - 酮的合成。4 - 氟苯基衍生物在小鼠或大鼠中表现出显著的镇痛、抗炎和解热活性，以及在体外与乙酰水杨酸相当的血小板抗聚集活性。
