SYNTHESIS, ANTIMICROBIAL ACTIVITY, α-AMYLASE INHIBITORY TESTS AND MOLECULAR DOCKING STUDIES OF THIAZOLE BASED HYDRAZONES DERIVED FROM 2-ACYL-(1H)-INDENE-1,3(2H)-DIONES

A series of new thiazole based hydrazones have been synthesized and their antimicrobial and alpha-amylase (type-II diabetes) inhibitory activities have been evaluated. The structures of synthesized derivatives were elucidated by various spectral techniques including FTIR, NMR and mass spectrometry. Antibacterial activity tests were performed against two Gram-positive (Bacillus subtilis and Staphylococcus aureus) and two Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacterial strains. Two fungal strains (Candida albicans and Aspergillus niger) were taken for testing antifungal activity. Among the tested derivatives, compound 3d was found to be the most potent against all tetsed bacterial and fungal strains. The alpha-amylase inhibitory activity of all compounds was also assayed using the starch iodine method. Derivatives 3j and 3k exhibited the best inhibitory activity against alpha-amylase enzyme with IC50 values of 0.26 +/- 0.06 and 0.32 +/- 0.02 mu M, respectively, in comparison to acarbose (IC50 = 0.11 +/- 0.00 mu M) as standard reference. The results of the biological activity evaluation were confirmed by docking studies.