4,4a,5,6-四氢-4a-取代苯并(h)噌啉-3(2H)酮的合成与药理研究
Synthesis and pharmacological study of 4,4a,5,6-tetrahydro-4a-substituted-benzo(h)cinnolin-3(2H)ones.
作者信息
Barlocco D, Pinna G A, Carboni L, Cipolla P
机构信息
Istituto Chimico Farmaceutico e Tossicologico, Università di Milano, Italy.
出版信息
Farmaco. 1989 Oct;44(10):967-74.
A series of 4,4a,5,6- tetrahydro-4a-substituted-benzo(h)cinnolin-3(2H)-one (II a-e) (III a) were synthesized and evaluated pharmacologically in comparison with the 4a-unsubstituted congeners (I), which were reported to be potent antithrombotic and antihypertensive agents. All the test compounds, apart from (II e) (R2 = OCH3) and (III a) (R1,R2 = H), displayed significant antihypertensive activity. In particular (II a) (R1,R2 = H) was more active than the unsubstituted analogue (I a). Moreover (II d) (R1 = OCH3), (II e) (R2 = OCH3) and (III a) showed antithrombotic activity comparable to or higher than that of ASA.
合成了一系列4,4a,5,6-四氢-4a-取代苯并(h)噌啉-3(2H)-酮(II a - e)(III a)，并与据报道为强效抗血栓和抗高血压药物的4a-未取代同系物(I)进行了药理学评估。除了(II e)(R2 = OCH3)和(III a)(R1,R2 = H)之外，所有测试化合物均表现出显著的抗高血压活性。特别地，(II a)(R1,R2 = H)比未取代类似物(I a)更具活性。此外，(II d)(R1 = OCH3)、(II e)(R2 = OCH3)和(III a)显示出与阿司匹林相当或更高的抗血栓活性。
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