Background: Hypertension is a complex and multifactorial disorder that is
an important cause of morbidity and mortality in all around the world; and the rationalized structural modification of
drugs represents an important strategy for to develop new antihypertensive drugs. Objective: To determine the vasorelaxant
effect of 4H-pyranes and 2-pyridones derivatives designed from nifedipine and milrinone as pharmacophoric scaffolds.
Methods: The vasorelaxant effect of all designed and synthesized compounds were carried out on the contraction
induced by noradrenaline 0.1 µM in isolated rat aorta rings. Results: Compounds 4a—j, 6a-c and 8a-c showed a concentration–
dependent and endothelium-independent relaxation on contraction induced by noradrenaline in isolated rat aorta
rings. Compounds 6a, 8a, 8b, and 8c were the most potent compounds of entire series evaluated; however, were less potent
than nifedipine and carbachol used as positive controls. Conclusions: Some compounds were designed and synthesized
with significant vasorelaxant effect which can be used for the development of new antihypertensive drugs.
Keywords: 4H-pyrans, 2-pyridones, antihypertensive, drug design, hypertension, vasorelaxant.
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