Cignarella G, Barlocco D, Landriani L, Folloni M, Pinna G A, Sala F, Germini M
Istituto Chimico Farmaceutico e Tossicologico, Università di Milano, Italy.
Farmaco Sci. 1988 Feb;43(2):169-79.
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).
已合成了具有抗高血压和抗血栓形成作用的7-氨基-(I b)和7-乙酰氨基-4,4a-二氢-5H-茚并(1,2-c)哒嗪-3-酮(I c)的新同系物，并进行了药理评价。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)相似的抗高血压作用，尽管持续时间较短。发现六种化合物的抗血栓活性与乙酰水杨酸相当或更高。特别是，(I l)和(I m)能像参比化合物(I c)一样完全保护小鼠免受血栓形成。
