International Journal of Pharmaceutical Chemistry and Analysis
  • Year: 2015
  • Volume: 2
  • Issue: 4

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

  • Author:
  • Palaniappan Senthilkumar1, Kullampalayam Krishnasamy Sivakumar1,, Gayam Krishnareddy1, Sanju Kaladharan2
  • Total Page Count: 12
  • Page Number: 170 to 181

1Department of Pharmaceutical Chemistry, KMCH College of Pharmacy, Kovai Estate, Tamil Nadu

2Department of Pharmacology, KMCH College of Pharmacy, Kovai Estate, Tamil Nadu

*Corresponding Author: Email: sivaveni2004@gmail.com

Online published on 28 July, 2016.

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 showed 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.

Keywords

Pyrazolone, Antibacterial, Antifungal, Shikimate kinase inhibitor