Author(s):
Hemanth Sudheer Kumar K, Parameshwar H
Email(s):
hemanthsudheer3@gmail.com
DOI:
10.5958/0974-360X.2018.00570.X
Address:
Hemanth Sudheer Kumar K1*, 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
Published In:
Volume - 11,
Issue - 7,
Year - 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.
Cite this article:
Hemanth Sudheer Kumar K, Parameshwar H. Synthesis, Molecular docking and Antibacterial Evalution of some Novel N-4 Piperzinyl derivatives of 8-Methoxy Grepafloxacin. Research J. Pharm. and Tech 2018; 11(7): 3103-3112. doi: 10.5958/0974-360X.2018.00570.X
Cite(Electronic):
Hemanth Sudheer Kumar K, Parameshwar H. Synthesis, Molecular docking and Antibacterial Evalution of some Novel N-4 Piperzinyl derivatives of 8-Methoxy Grepafloxacin. Research J. Pharm. and Tech 2018; 11(7): 3103-3112. doi: 10.5958/0974-360X.2018.00570.X Available on: https://rjptonline.org/AbstractView.aspx?PID=2018-11-7-69