Nitrothiazole-Thiazolidinone Hybrids: Synthesis and in Vitro Antimicrobial Evaluation

Chem Biodivers. 2022 Nov;19(11):e202200729. doi: 10.1002/cbdv.202200729. Epub 2022 Oct 6.

Abstract

Herein we report the synthesis of novel compounds inspired by the antimicrobial activities of nitroazole and thiazolidin-4-one based compounds reported in the literature. Target compounds were investigated in vitro for antitubercular, antibacterial, antifungal, and overt cell toxicity properties. All compounds exhibited potent antitubercular activity. Most compounds exhibited low micromolar activity against S. aureus and C. albicans with no overt cell toxicity against HEK-293 cells nor haemolysis against human red blood cells. Notably, compound 3b exhibited low to sub-micromolar activities against Mtb, MRSA, and C. albicans. 3b showed superior activity (0.25 μg/ml) against MRSA compared to vancomycin (1 μg/ml).

Keywords: 5-nitrothiazoles; ESKAPE pathogens; antimicrobial; molecular hybridization; thiazolidine-4-ones.

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents* / pharmacology
  • Antitubercular Agents / pharmacology
  • Candida albicans
  • HEK293 Cells
  • Humans
  • Microbial Sensitivity Tests
  • Staphylococcus aureus*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antitubercular Agents