Design, Synthesis and ex vivo Study of the Vasorelaxant Activity Induced by Isosteric Derivatives of Dihydropyridines (NH→O)

Title:Design, Synthesis and ex vivo Study of the Vasorelaxant Activity Induced by Isosteric Derivatives of Dihydropyridines (NH→O)

Volume: 13 Issue: 5

Author(s): Priscila Rendón-Vallejo, Samuel Estrada-Soto, Miguel A. Vázquez, Fernando Hernández- Borja, Rafael Villalobos-Molina and Maximiliano Ibarra-Barajas

Affiliation:

Keywords: 4H-pyrans, 2-pyridones, antihypertensive, drug design, hypertension, vasorelaxant.

Abstract: 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.

Cite this article as:

Rendón-Vallejo Priscila, Estrada-Soto Samuel, A. Vázquez Miguel, Hernández- Borja Fernando, Villalobos-Molina Rafael and Ibarra-Barajas Maximiliano, Design, Synthesis and ex vivo Study of the Vasorelaxant Activity Induced by Isosteric Derivatives of Dihydropyridines (NH→O), Letters in Drug Design & Discovery 2016; 13 (5) . https://dx.doi.org/10.2174/1570180812666151003002501