ORIENTAL JOURNAL OF CHEMISTRY
www.orientjchem.org
An International Open Access, Peer Reviewed Research Journal
ISSN: 0970-020 X
CODEN: OJCHEG
2019, Vol. 35, No.(4):
Pg. 1248-1253
This is an Open Access article licensed under a Creative Commons license: Attribution 4.0 International (CC- BY).
Published by Oriental Scientific Publishing Company © 2018
Synthesis of Fluoroquinolones derivatives as Antimicrobial Agents
LUBNA SWELLMEEN
1
*, AMAL UZRAIL
2
, RAND SHAHIN
3
and YUSUF AL-HIARI
4
1
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Zarqa University, Jordan.
2
Department of Medical Analysis, Faculty of Allied Medical Sciences, Zarqa University, Jordan.
3
Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Hashemite University, Jordan.
4
Faculty of Pharmacy, The University of Jordan, Amman 11942, Jordan Zarqa.
*Corresponding author E-mail: lswellmeen@zu.edu.jo
http://dx.doi.org/10.13005/ojc/350401
(Received: April 08, 2019; Accepted: August 05, 2019)
ABSTRACT
Fluoroquinolones are well known to have an anti-infective action. In the present study we
have described the synthesis of novel florouquinolones derivative as antimicrobial agent. The
biological test highlighted a good inhibitory activity for the 7-Chloro-1-Alkyl-6-fluoro-8-nitro-4-oxo-1,
4-dihydroquinoline-3-carboxylic acid derived synthons especially against pathogenic Gram-negative
bacteria (Pseudomonas aeruginosa) and Gram-positive bacteria (Staphylococcus aureus and
Streptococcus agalactiae). The binding interactions were monitored and could explain the good
inhibitory activity of the synthesized derivatives of florouquinolones.
Keywords: Florouquinolones derivatives, Antibacterial activity, Gram-negative bacteria and
Gram-positive bacteria.
INTRODUCTION
Anti-infective agents played a major
role in saving human lives. Among these agents
are the fluoroquinolones class, which had risen
to be highly appreciated, especially if there was
microbial resistance against penicillin and macrolide.
Fluoroquinolone pharmacophore (Fig. 1) is well
known to have antibacterial activity, and since
1980 there were many generation introduced to
the market
1
. The fluoroquinolones were found to be
effective to combat urinary tract infection
1
ideal in
treating Neisseria gonorrhea
1
and highly effective
to treat tuberculosis
2
. In addition, fluoroquinolone
nucleus are presented widely in biologically active
compounds such as PDE 4 inhibitors
3
, PIM kinase
inhibitors
4
, GSK β inhibitors
5
.
Fig. 1. Fluoroquinolone general formula
The encouraging properties of
fluoroquinolones such as; broad spectrum of activity,
good oral bioavailability, good tissue penetrability
and low incidence of adverse effect
6
gave them
high appreciation and encouraged researcher to