Design, Synthesis and Antibacterial Study of New Agents Having 4-Thiazolidinone Pharmacophore

Abstract

A New series of compounds containing 4-thiazolidinone pharmacophore 5(a-d) have been synthesized. The chemical structure of the intermediate and final compounds was characterized and confirmed by using FT-IR and 1 H-NMR spectroscopy. All final compounds were tested against gram-positive and gram-negative bacteria using a well-diffusion technique for their ability as antimicrobial agents. The tested compounds 5b and 5c showed comparable antibacterial activity against gram-negative bacteria and gram-positive bacteria like escherichia coli, Acinetobacter bumannii, Staphylococcus aureus, and Streptococcus pyougenes as a standard drug compared with Trimethoprim. Molecular docking simulations were studied to understand the molecular core. The results were achieved by docking, the most active compounds into the active site of protein of the bacteria which completely accorded with in vitro results.

Potential Nitrogen-Based Heterocyclic Compounds for Treating Infectious Diseases: A Literature Review

“…In contrast, compound 491 had preferable activity than the standard drug on S. pyogenes and was equivalent to the trimethoprim in Acinetobacter baumanni. From the comparison of antibacterial results, it was explained that among the tested compounds, compound 492 showed the best activity as compared to 491 [ 50 ] . The 4-thiazolidinones derivatives based on 1,2,4-triazole ( 497 – 506 ) were reported by Ahmed et al, 2016 ( Scheme 41 ).…”

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

“…Among the 3-amino-2-aryl/alkylthiazolidin-one derivatives, Compound 115 (Figure 50) showed higher inhibitory activity (inhibition zone -8-17 mm) than standard chloramphenicol (5-15 mm) to concentration 150 µg/mL against all tested strains (Proteus vulgaris, E. coli, K. pneumoniae, P. aeruginosa and S. aureus) [122]. Among the series of 116a-116d, Compound 116c with chloro substituent showed the antibacterial activity against E. coli practically equivalent to trimethoprim and better than trimethoprim against Acinetobacter baumannii and Streptococcus pyogenes [123]. The biphenylbased thiazolidine-4-ones (117a-117c) showed good antimicrobial against bacterial (E. coli, S. aureus, B. subtilis) and fungal (A. niger, C. albicans) strains, except 117c that exhibited moderate effect against fungal strains [124].…”