SYNTHESIS OF NOVEL [2-(2-(4-HALO SUBSTITUTED PHENYL) QUINOLINE-4-CARBONYL)-5-METHYL-4-(2- PHENYLHYDRAZINEYLIDENE)-2,4-DIHYDRO-3H-PYRAZOL3-ONE] HYBRIDS AND ITS PHARMACOLOGICAL STUDIES
In this paper, we describe the synthesis of integrated pyrazole derivatives carrying quinolone moiety by conventional technique. Pyrazole derivatives were synthesized by condensation of hydrazide and ethyl-3-oxo-2-(2- phenylhydrazilidiene) butanoate. Fourier transforms infrared (FT-IR), 1H- Nuclear magnetic resonance, 13C-Nuclear magnetic resonance (NMR), and liquid chromatography-mass spectrometry (LCMS) studies were used to confirm the structure of the compounds. Docking studies were carried out against the antimicrobial target to know the interaction of the molecules (ligands) with the docked target. Among the docked compounds pyrazole derivative brominated compounds 4d, 4e, 4f, 4g, and 4h violated Lipinski’s Rule of Five and thus were not suitable leads. Comparing the synthetic compounds 4c, 4g, and 4i to the reference drug ofloxacin, they exhibit excellent antibacterial activities.
Readers around the world
