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Keywords:

  • vasodilators;
  • dihydropyridazin-3(2H)-one;
  • hypertension

Abstract

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.