New congeners of antihypertensive and antithrombotic 7-amino or 7-acetyl-aminosubstituted-4,4a-dihydro-5H-indeno (1,2-c)pyridazin-3-ones.

Il Farmaco; edizione scientifica Pub Date : 1988-02-01
G Cignarella, D Barlocco, L Landriani, M Folloni, G A Pinna, F Sala, M Germini
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Abstract

New congeners of the antihypertensive and antithrombotic 7-amino-(I b) and 7-acetylamino-4,4a-dihydro-5H-indeno(1,2-c)pyridazin-3-one (I c) have been synthesized and evaluated pharmacologically. Compounds (I k) (R = 7-NHCH3), (I l) (R = 7-N(CH3)COCH3) and (I m) (R = 7-N(CH3)COC2H5) exhibited an antihypertensive effect similar to that of (I b) and (I c), though short lasting. The antithrombotic activity of six compounds was found comparable to or higher than that of acetylsalicilic acid. In particular, (I l) and (I m) fully protected mice against thrombosis, as did the reference compound (I c).

抗高血压和抗血栓的7-氨基或7-乙酰氨基取代-4,4 -二氢- 5h -吲哚(1,2-c)吡啶嗪-3-酮的新同源物。
合成了抗高血压和抗血栓的7-氨基-(I b)和7-乙酰氨基-4,4 -二氢- 5h -吲哚-(1,2-c)吡啶嗪-3-酮(I c)的新同源物,并对其进行了药理学评价。化合物(I k) (R = 7-NHCH3)、(I l) (R = 7-N(CH3)COCH3)和(I m) (R = 7-N(CH3)COC2H5)表现出与(I b)和(I c)相似的降压作用,但持续时间较短。发现六种化合物的抗血栓活性与乙酰水杨酸相当或高于乙酰水杨酸。特别是,(I 1)和(I m)完全保护小鼠免受血栓形成,参考化合物(I c)也是如此。
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