Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro

Abstract

Quinolones are among the prominent class of broad-spectrum antibiotics. In this work, a series of 1,4-dihydro-4-oxo-3-[3-{benzenesulfon}-2-hydrazino-1-oxo-]quinoline derivatives 6a-e were synthesized and tested for their antibacterial efficacy in vitro. Compounds 6a-e were characterized by NMR (1H,13C), HRMS and IR analysis. All these compounds confirmed bactericidal activity against tested bacterial strains. The MIC data have shown that compounds 6e (MIC = 7.5 mg/mL) displayed better activity against Staphylococcus aureus, Escherichia coli (ETEC) and Pseudomonas aeruginosa. Compounds 6b-e (MIC = 7.5 mg/mL) have similar activity as Norfloxacin against E. coli. Molecular docking studies was also conducted to explore binding interactions of our compounds at the active sites of the GyrB subunit of E. coli K-12.

Keywords

• Quinolones
• Hydrazine
• Benzene sulfonyl chloride
• Molecular Docking