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6-(取代苯基)-5-羟甲基-4,5-二氢-3(2H)哒嗪酮的抗高血压和抗血栓形成活性

Antihypertensive and antithrombotic activities of 6-(substituted phenyl)-5-hydroxymethyl-4,5-dihydro-3(2H)pyridazinones.

作者信息

Barlocco D, Martini A, Pinna G A, Curzu M M, Sala F, Germini M

机构信息

Istituto Chimico Farmaceutico e Tossicologico Università di Milano, Italy.

出版信息

Farmaco Sci. 1987 Aug;42(8):585-94.

PMID:3666129
Abstract

The synthesis of a series of 6-(4R-phenyl)-5-hydroxymethyl-4,5-dihydro-3(2H)pyridazinones is reported. The compounds were evaluated for their oral antihypertensive activity in rats and some of them [(V b), R = NH2] and [(V c), R = NHCOCH3] were found to induce a high decrease in systolic blood pressure. Moreover all the compounds displayed an antithrombotic activity comparable to, or greater than, that of ASA.

摘要

报道了一系列6-(4R-苯基)-5-羟甲基-4,5-二氢-3(2H)哒嗪酮的合成。对这些化合物在大鼠体内的口服抗高血压活性进行了评估,发现其中一些化合物[(V b),R = NH2]和[(V c),R = NHCOCH3]可使收缩压大幅下降。此外,所有化合物均表现出与阿司匹林相当或更强的抗血栓活性。

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