Vol. 7, Issue 11 (2018)

Author(s):
Arun Kumar

Abstract:
This study reports the synthesis and characterization of a novel series of substituted-2-aminothiazole derivatives (6a-6o) through a multi-step synthetic approach. The structural confirmation of these compounds was accomplished using spectroscopic techniques, including proton nuclear magnetic resonance (¹H-NMR), mass spectrometry, and FTIR spectroscopy. The synthesized derivatives were evaluated for their antibacterial and antifungal activities against key microbial strains, including Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Aspergillus niger, Mucor purpureus, and Aspergillus flavus, using the agar diffusion method. The antibacterial screening revealed that compounds exhibit prominent anti E. coli growth inhibiting activity at conc. of 12.5 and 25 µg/mL specially thiazoles 6e, and 6a, 6d, 6k, 6l and 6n. The compounds were moderately effective in controlling the growth of S. aureus and P. auroginosa. The antifungal activity shows that none of the compound from the series (6a-6o) had antifungal activity at conc. of 12.5 or 25 µg/mL, which suggest that all the compounds were found to be poorly active. In-silico ADME and toxicity studies revealed that compounds are fairly compatible and were devoid of potential toxicity except hepatotoxicity and immunotoxicity. The docking studies on DNA gyrase (PDB ID; 1KZN) shows favourable binding interaction comparable to the pre occupied ligand Clorobiocin.