Synthesis, Docking and Antihypertensive Activity of Pyridone Derivatives

Abstract

A substituted 4-((5-cyano-1-ethyl-2-hydroxy-4-methyl-6-oxo-1,6-dihydropyridin-3-yl)diazenyl)benzene-sulfonamides were picked up via coupling of aromatic Diazonium salt for sulfonamide derivatives on 3-cyano-6-hydroxyl-2-pyridone derivative. The synthesized 4-((pyridinyl)azo)benzene-sulfonamide analogues have been evidenced through elemental and spectral analyses "FT-IR, 1 HNMR, 13 CNMR and MS". The produced derivatives were exposed to molecular docking to predict their antihypertensive activity toward protein databank identification number (PDB ID 6JP5) complexed with an amino acids consequent from the human Voltage-dependent L-type calcium channel (LCC) alpha-1S subunit. The docking studies outcomes endorsed us to utilize these analogues in vivo antihypertensive effectiveness treatise. The Mean systolic blood pressure (SBP) of hypertensive rats injected by Dihydropyridine derivatives (DHPD) were evaluated in comparable with nifedipine that utilized as standard drug. Moreover, the vasorelaxant effectiveness of the synthesized derivatives 7 a-e were examined against the contraction induced by noradrenaline (0.1 mM, NA) on aorta rat rings.

Potential application of bisoprolol derivative compounds as antihypertensive drugs: synthesis and in silico study

“…Here, positive values indicate stronger bond strength between the ligands and the receptor's binding pocket. Despite the positive values, the binding energy range aligns with previous studies investigating the potential of compounds as antihypertensive drugs based on binding energy values [4,12,13]. These studies used different ligands and receptors, but their results demonstrated similar value ranges for binding energy, indicating their activity as potential antihypertensive agents.…”

“…In addition to combination therapies, the development of antihypertensive drugs can also involve the synthesis of derivative compounds. For instance, Masaret et al [12] successfully developed antihypertensive drug compounds by synthesizing pyridone derivatives. Furthermore, there have been advancements in the development of antihypertensive drug compounds through synthesis and molecular docking methods.…”

“…For instance, Masaret et al . [ 12 ] successfully developed antihypertensive drug compounds by synthesizing pyridone derivatives. Furthermore, there have been advancements in the development of antihypertensive drug compounds through synthesis and molecular docking methods.…”

New pyridine and chromene scaffolds as potent vasorelaxant and anticancer agents

“…A literature survey has reported that many pyridine derivatives play a vital role in vasorelaxation therapeutics. 15 For example, milrinone and amrinone are positive inotropic agents with vasodilator properties; nifedipine is a peripheral and coronary vasodilator drug of the calcium channel blockers. [15][16][17] Furthermore, different pyridine-3-carbonitrile analogs I, II and different nicotinate esters such as micinicate, hepronicate and inositol nicotinate have emerged as signicant vasodilating agents (Fig.…”

Sulfonamides with Heterocyclic Periphery as Antiviral Agents

“…N-heterocycles and linear products synthesized from sulfonamides or containing a sulfonamide fragment in the side chain are important objects for studying biological activity. Traditionally, sulfonamides are primarily considered as antibacterial agents; however, among these substances one can find not only effective antibiotics [1,2], but also compounds with very different activities: oral hypoglycemic [3,4], antitumor [3,5], antiviral [6][7][8][9], antiepileptic [10], antihypertensive [11], antiprotozoal [12], antifungal [13], anticancer [14][15][16], anti-inflammatory [17], diuretic [18], butyrylcholinesterase inhibitors (anti-Alzheimer's disease activity) [19], MAO-B specific inhibitors (activity in the treatment of neurodegenerative disorders such as Parkinson's disease) [20], COX-2 inhibitors (therapy of inflammatory disease) [21], etc. Recent advances in the medicinal chemistry of sulfonamides showed the possibilities of new unique drug design.…”