Synthesis, Characterization, in vitro Biological Evaluation of a Series of Benzothiazole Amides as Antibacterial Agents

Abstract

A series of benzothiazole amides (VH01-06) were synthesized by using modified Schotten-Baumann reaction conditions, all the resultant compounds were obtained in good yields and purity. The molecular structure of the compounds was characterized using physical and spectral methods. The structures of the compounds were consistent with the analytical data obtained for FT-IR, 1H NMR, 13C NMR and HRMS ESI-Mass spectroscopic techniques. Further, compounds were subjected to the in vitro antibacterial activity screening against various strains that includes Gram-positive bacteria (methicillin-resistant Staphylococcus aureus (MRSA) ATCC 3359 and methicillin-sensitive Staphylococcus aureus (MSSA) ATCC 2592) and Gram-negative bacteria (Escherichia coli J53 R1, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 10031 and Klebsiella pneumonia BAA-1075). Based on the biological screening results, compounds VH01-06 were found to possesses limited antibacterial properties against selected strains, since the recorded activity was found at 100 µM concentration. While compound VH05 displayed specific activity against E. coli ATCC 25923 at 200 µg/mL.