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2020 Volume 11 Issue 3

Design, Synthesis, Docking Study and Preliminary Pharmacological Assessment of New Norfloxacin Analogues Having Thiazole Nucleus


Nawal T. Ajjah, Noor H. Naser, Akeel A. Abo Alard, Muslim F. Diwan
Abstract

Bacterial resistance is the most dangerous and critical problem associated with the use of antibiotics, due to the uncontrolled and miss use of many types of them. Fluoroquinolones are a class of antibacterial agents that possess an anti-inflammatory effect in addition to their antibacterial effect, and they are resisted by many species of microorganisms through different mechanisms. It was found that increase bulkiness at C7 of fluoroquinolones moiety will reduce bacterial resistance by reducing the effect of the efflux pump, and it was also reported that this modification will improve anti-inflammatory activity. So, thiazole ring and a group of its derivatives (which possess antibacterial and anti-inflammatory activity) were incorporated into a secondary amine at the piperazine ring of norfloxacin. Using FT-IR spectroscopy, 1H-NMR spectral, and some physical-physiochemical properties, the synthesized compounds were confirmed and characterized for their chemical structures. In vivo, an acute anti-inflammatory effect of compounds, III and IVa-f, was estimated using the paw-edema model in rats. Norfloxacin 20mg/kg, and diclofenac sodium 3mg/kg were employed as reference drugs. All tested compounds exhibited significant (p<0.05) reduction in the paw edema when compared to the control group (propylene glycol (PG)). In in-vitro, the antibacterial effect of all synthesized compounds was evaluated via the use of the agar-well diffusion method (AWD). The antibacterial study was shown a topmost inhibition zone for the compound III against E. coli and the lowest inhibition zone for the compound IVd against Staphylococcus aureus. Docking studies showed the affinity of the synthesized compounds toward the topoisomerase enzyme.


How to cite this article
Ajjah N T, Naser N H, Alard A A A, Diwan M F. Design, Synthesis, Docking Study and Preliminary Pharmacological Assessment of New Norfloxacin Analogues Having Thiazole Nucleus. J Biochem Technol 2020;11(3):58-67
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J BIOCHEM TECH
J BIOCHEM TECH
Journal of Biochemical Technology is a peer reviewed International Journal published by the Sevas Publishing on behalf of the Biochemical Technology Society, a Registered Charity Organization from India

AREA OF INTEREST
AREA OF INTEREST
Areas of high interest, cover new advances in enzymatic and protein mechanims; applied molecular genetics and biotechnology; genomics and proteomics; metabolic; medical, environmental, food and agro biotechnology.

FOCUS AND SCOPE
FOCUS AND SCOPE
Journal Of Biochemical Technology” Provides A Medium For The Rapid Publication Of Full-Length Articles, Mini-Reviews Of New And Emerging Products And Short Communications On All Aspects Of ...

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This journal provides immediate open access to its content on the principle that making research freely available to the public supports a greater global exchange of knowledge. Keywords include, Biochemical Research: Endo/exocytosis, Trafficking, Membrane Biology, Cell Migration, Cell-Matrix Organelle Biogenesis, Cytoskeleton Proteolysis, Cell Death, Cell Cycle, Cancer, Cell Growth/Death, Differentiation, Drug Targets, Gene Therapy, Models of Disease, Proteomics, Stem Cells, Bioenergetics, Mitochondria, Free Radicals, Redox Signaling, Ion Transport/Channels, Oxidative