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具有血小板抗聚集及其他活性的N-酰基-4,7,7-三甲基-N-苯基-3-(1-哌啶基或二甲基氨基)双环[2.2.1]庚-2-烯-2-硫代酰胺

N-acyl-4,7,7-trimethyl-N-phenyl-3-(1-piperidinyl or dimethylamino)bicyclo[2.2.1]hept-2-ene-2-carbothioamides with platelet antiaggregating and other activities.

作者信息

Ranise A, Bruno O, Bondavalli F, Schenone P, D'Amico M, Falzarano C, Filippelli A, Lampa E

机构信息

Istituto di Scienze Farmaceutiche dell'Universitá Viale Benedetto XV, Genova, Italy.

出版信息

Farmaco. 1993 Apr;48(4):551-65.

PMID:8102849
Abstract

A series of N-acyl-4,7,7-trimethyl-N-phenyl-3-(1-piperidinyl or dimethylamino)bicyclo[2.2.1]hept-2-ene-2-carbothioamides was prepared in excellent yields by reaction of 4,7,7-trimethyl-N-phenyl-3-(1-piperidinyl or dimethylamino)bicyclo[2.2.1]hept-2-ene-2-carbothioamides with a number of aromatic or heterocyclic acyl chlorides in dry pyridine solution and in the presence of sodium hydride. Some of the above compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid; moreover, some compounds exhibited moderate analgesic, antiinflammatory and hypotensive activities in mice or rats.

摘要

通过使4,7,7-三甲基-N-苯基-3-(1-哌啶基或二甲基氨基)双环[2.2.1]庚-2-烯-2-硫代甲酰胺与多种芳族或杂环酰氯在干燥吡啶溶液中并在氢化钠存在下反应,以优异的产率制备了一系列N-酰基-4,7,7-三甲基-N-苯基-3-(1-哌啶基或二甲基氨基)双环[2.2.1]庚-2-烯-2-硫代甲酰胺。上述一些化合物在体外显示出优于或与乙酰水杨酸相当的血小板抗聚集活性;此外,一些化合物在小鼠或大鼠中表现出适度的镇痛、抗炎和降压活性。

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