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International Journal of Pharmaceutical Chemistry and Analysis


Design and Microwave Assisted Synthesis of Chalcone of N-(4,5-Dihydro-5-oxo-1H-Pyrazol-3-yl)Acetamide: Antimicrobial Properties evaluation and Docking study as Shikimate Kinase Inhibitors


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Author Details: Palaniappan Senthilkumar, Kullampalayam Krishnasamy Sivakumar, Gayam Krishnareddy, Sanju Kaladharan

Volume : 2

Issue : 4

Online ISSN : 2394-2797

Print ISSN : 2394-2789

Article First Page : 170

Article End Page : 181


Abstract

Eight hybridized pyrazolone analogs were designed, docked, synthesized by microwave technique and evaluated for their in-vitro antimicrobial property against four Gram positive, four Gram negative bacterial strains and two fungal strains. Chalcone derivatives of pyrazolone moiety 5a, 5b, 5f, 5g and 5h shows good antibacterial activity aganist Gram positive strains (Percentage zone of inhibition range 68 to 100% with MIC range 12.5-50 μg/mL) compared with Ciprofloxacin (bacteria) and Clotrimazole (fungal). Compound 5h showed good binding at the active site of the protein with docking score -8.69 and  shows hydrogen bonding with Arg 58, Arg 136 and electronic interactions with Asp 34, Glu 38. All other compounds shows mild to moderate activity against all the screened micro-organisms tested.

Key Words:
Pyrazolone, Antibacterial, Antifungal, Shikimate kinase inhibitor