| Summary: | In this manuscript, we describe the design, preparation, and studies of antimicrobial activity of a series of novel heteroarylated benzothiazoles. A molecular hybridization approach was used for the designing compounds. The in vitro evaluation exposed that these compounds showed moderate antibacterial activity. Compound <b>2j</b> was found to be the most potent (MIC/MBC at 0.23–0.94 mg/mL and 0.47–1.88 mg/mL) On the other hand, compounds showed good antifungal activity (MIC/MFC at 0.06–0.47 and 0.11–0.94 mg/mL respectively) with <b>2d</b> being the most active one. The docking studies revealed that inhibition of <i>E. coli MurB</i> and 14-lanosterol demethylase probably represent the mechanism of antibacterial and antifungal activities.
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