Preclinical Research
As part of a research program to identify compounds with potent antihypertensive properties, a new series of dihydropyridazin‐3(2H)‐one analogs was synthesized and evaluated for vasodilator activity in rat thoracic aortic rings. Most of the newly synthesized compounds displayed good vasorelaxant activity as compared with SK&F‐93741 and hydralazine, with the N2‐unsubstituted 4‐isobutyramidophenylpyridazinone derivative 5 being the most potent vasorelaxant, producing vasorelaxation greater than that of hydralazine and equipotent to SK&F‐93741. A significant effect of the 6‐phenyl substituents and substitution at N‐2 position of pyridazinone nucleus on the vasodilatory activity was observed.