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Abstract

DESIGN, SYNTHESIS & EVALUATION OF NOVEL SUBSTITUTED FLUOROQUINOLONE-BENZIMIDAZOLE ANTIBACTERIALS

*Shital J. Patil, Dr. Ashok P. Pingle, Khudabaksha Tamboli.

ABSTRACT

The current developments of the chemical and biological aspects of fluoroquinolones in a chronological manner touching upon their antibacterial properties based on the structure- activity relationship while pointing out to their mode of action. . Out of more than 8000 analogues of fluoroquinolones synthesized bearing variety of ring systems, a few dozen have been established in the market, and more are in the horizon to be introduced. Bacterial resistance to fluoroquinolones is seriously challenging the clinical applications of this class of antimicrobial agent. Most of the fluoroquinolones currently on the market or under development have only moderate activity against many gram-positive cocci, including staphylococci and streptococci. Fluoroquinolones effectiveness is concentration-dependant. It has been shown that in order for bacteria to be highly susceptible to Fluoroquinolones and prevent resistant mutants, the maximum concentration must be 10 times that of the minimum inhibitory (MIC) concentration when treating against gram-positive bacteria. The antibacterial activity of some substituted Benz imidazole derivatives against Gram negative bacteria Escherichia coli was investigated.

Keywords: Fluoroquinolones, Antibacterial, Gram-positive, Resistant mutants, Benzimidazole.


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