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Abstract <p>A series of ciprofloxacin-based thiazolidinone derivatives were developed and prepared by reacting active methylene compound with corresponding aldehydes. The novel compounds were analyzed using several spectroscopic techniques (FT-IR, <sup>1</sup>H, <sup>13</sup>C NMR and MS), and their antimicrobial properties were tested. Their minimum inhibitory concentration values were between 1.6 and 72.1 µg/mL, similar to MXF (1.9–3.5 µg/mL). From screening, the antibacterial results showed that <i>p</i>-chlorobenzylidene, <i>p</i>-dimethylaminobenzylidene, and <i>m</i>-methoxybenzylidene derivatives showed outstanding antibacterial activity against <i>E. coli</i> with zone of inhibition values of 27±0.1, 21±0.1, and 22±0.3 mm, respectively. The molecular docking predictions showed that the most active compounds have good binding affinities with <i>E. coli</i> DNA gyrase (7C7N). ADMET predictions were performed; the most thiazolidines possess the highest drug likeness score (1.23–1.61) as a promising pharmacokinetic safety profile.</p>

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New 4-Thiazolidinone-Bearing Fluoroquinolone Derivatives: Synthesis, Antimicrobial Effectiveness, Structural Characterization, and In Silico Docking Analysis

  • 期刊论文

  • 发表日期：

    2025年3月27日

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  • V. S. P. K. Gudapati,
  • S. R. Basireddy,
  • D. V. P. K. Gudapati,
  • M. Afzal,
  • A. Ayub,
  • S. K. Kolli

摘要

Abstract

A series of ciprofloxacin-based thiazolidinone derivatives were developed and prepared by reacting active methylene compound with corresponding aldehydes. The novel compounds were analyzed using several spectroscopic techniques (FT-IR, 1H, 13C NMR and MS), and their antimicrobial properties were tested. Their minimum inhibitory concentration values were between 1.6 and 72.1 µg/mL, similar to MXF (1.9–3.5 µg/mL). From screening, the antibacterial results showed that p-chlorobenzylidene, p-dimethylaminobenzylidene, and m-methoxybenzylidene derivatives showed outstanding antibacterial activity against E. coli with zone of inhibition values of 27±0.1, 21±0.1, and 22±0.3 mm, respectively. The molecular docking predictions showed that the most active compounds have good binding affinities with E. coli DNA gyrase (7C7N). ADMET predictions were performed; the most thiazolidines possess the highest drug likeness score (1.23–1.61) as a promising pharmacokinetic safety profile.