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Synthesis and Pharmacological Evaluation of 6‐Arylpyridazinones as Potent Vasorelaxants
Author(s) -
Bansal Ranju,
Kumar Dinesh,
Sharma Deepika,
Calle Carmen,
Carron Rosalia
Publication year - 2013
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21079
Subject(s) - hydralazine , chemistry , vasodilation , pharmacology , vasodilator agents , chemical synthesis , stereochemistry , medicine , biochemistry , in vitro , blood pressure
AbstractPreclinical ResearchAs part of a research program to identify compounds with potent antihypertensive properties, a new series of dihydropyridazin‐3(2 H )‐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 N 2‐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.