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Research Journal of Pharmacy and Technology
Year : 2018, Volume : 11, Issue : 7
First page : ( 3103) Last page : ( 3112)
Print ISSN : 0974-3618. Online ISSN : 0974-360X.
Article DOI : 10.5958/0974-360X.2018.00570.X

Synthesis, Molecular docking and Antibacterial Evalution of some Novel N-4 Piperzinyl derivatives of 8-Methoxy Grepafloxacin

Kumar K Hemanth Sudheer1,*, Parameshwar H2

1School of Pharmacy and Medical Sciences, Singhania University, Pacheri Bari, Jhunjhunu, Rajasthan, India

2Professor and Head, Mother Teresa College of Pharmacy, Osmania University, Hyderabad, Telangana, India

*Corresponding Author E-mail: hemanthsudheer3@gmail.com

Online published on 31 October, 2018.

Abstract

Grepafloxacin, a fluroquinolones analogue has activity against a wide range of gram-negative and gram positive microorganisms by inhibiting the enzymes topoisomerase-II (DNA gyrase) and topoisomerase-IV which are required for bacterial DNA replication, transcription, repair and recombination. A series of 8-methoxy grepafloxacin derivatives were synthesized (P1-P10) Via N-Piperzinyl linkage. The structural conformation done by infra-red, nuclear magnetic resonance, mass spectrometry and elemental analysis technique. In present investigation, we screened docking stimulation for synthesized compounds (P1-P10) to find out binding modes of derivatives with 3FV5 and 3IMW. The compound P5 showed good antibacterial activity against gram positive (S. Aureus) and compound P3 and P6 showed good antibacterial activity against gram negative (E. Coli) in comparison with standard drugs (Ciprofloxacin and Grepafloxacin). The Zone of inhibition and MIC studies performed to synthesized compounds. The correlation between experimental data (minimum inhibition concentration) verses docking score suggest that penetration for docking simulation are mild in reproducing experimental orientation of these synthesized compounds.

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Keywords

N-Piperzinyl derivatives, Ciprofloxacin, 8-methoxy grepafloxacin, DNA gyrase, topoisomerase-IV, Docking studies.

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