Synthesis, antimicrobial, antiquorum-sensing and cytotoxic activities of new series of benzothiazole derivatives

New series of benzothiazole derivatives were designed and synthesized. The newly synthesized compounds were screened for their antibacterial activity against Escherichia coli, Staphylococcus aureus and Bacillus cereus. Compounds 6j and 6o showed the highest activity against E. coli and S. aureus. The antifungal activity of these compounds was also tested against Candida albicans and Aspergillus fumigatus 293. Compounds 4c, 4g and 6j exhibited the highest activity against C. albicans. In addition, compounds 4a and 6j displayed promising activity against A. fumigatus 293. The same compounds were examined for their antiquorum-sensing activity against Chromobacterium violaceum ATCC 12472, whereas compounds 4a, 6j and 6p showed moderate activity. The in vitro cytotoxicity testing of the synthesized compounds was performed against cervical cancer (Hela) and kidney fibroblast cancer (COS-7) cell lines. Results indicated that all tested compounds have IC50 values >50 μmol/L against both cell lines. Molecular properties, toxicities, drug-likeness, and drug score profiles of compounds 4a–c, 5a, 6g,h, 6j, 6l, 6o and 7c,d were also assessed.

Graphical abstractNew benzothiazole derivatives 4a–e, 5a–c, 6a–r and 7a–d were designed, synthesized and screened for their antimicrobial activity.Figure optionsDownload full-size imageDownload as PowerPoint slide