Barlocco D, Martini A, Pinna G A, Curzu M M, Sala F, Germini M
Istituto Chimico Farmaceutico e Tossicologico Università di Milano, Italy.
Farmaco Sci. 1987 Aug;42(8):585-94.
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.
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。