Synthesis, Docking and Antihypertensive Activity of Pyridone Derivatives
Ghada S. Masaret
Abstract
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.