Synthesis, Anti-Bacterial and Anti-biofilm Activity of New Iminothiazolidinones
Kumaraswamy Gullapelli *
Department of Chemistry, Mahatma Gandhi Institute of Technology, Hyderabad-500 075, India.
Ravichander Maroju
Department of Chemistry, Mahatma Gandhi Institute of Technology, Hyderabad-500 075, India.
*Author to whom correspondence should be addressed.
Abstract
Aim: Iminothiazolidinones are one of the important classes of heterocyclic compounds and they occupied unique position in medicinal chemistry due to their wide range of biological and pharmaceutical properties. In view this potential activity, it has been planned to synthesize a series of New Iminothiazolidinones on benzimidazole nucleus and to study their biological activity.
Methodology: Iminothiazolidinones and 1,1 dioxide- Iminothiazolidinones were synthesized with a simple and efficient method of cyclic condensation of aryl thiourea containing benzimidazole and thiazole with chloroacetic acid .This method requires mild reaction conditions, simple procedure and gives good yield.
Results: The structures of the synthesized compounds were assessed by Infrared, NMR and Mass spectroscopic methods. The synthesized compounds were screened for their antibacterial and biofilm inhibitory activities against selected multi drug resistant bacterial strains.
Conclusion: In accordance with the results obtained, growth inhibition was found significant with compounds 5d and 5e. Methicillin resistant Staphylococcus aureus (MRSA), Vancomycin resistant Enterococcus (VRE), and extended spectrum β‑lactamase (ESBL) producing Klebsiella pneumoniae have shown varied susceptibility towards these compounds. The Biofilm inhibition Concentrations (BFIC) of compounds 5e and 5d are 3.22 ±0.56 and 6.58 ±1.5 µg/mL respectively were noted against MRSA.
Keywords: Benzimidazole, iminothiazolidinones, anti-bacterial activity and anti-biofilm activity.