Benzothiazole‐Based‐Bioconjugates with Improved Antimicrobial, Anticancer and Antioxidant Potential

• Published in: ChemistrySelect (Weinheim) 2018-10, Vol.3 (40), p.11326-11332
• Main Authors: Kumari, Bhawana, Chauhan, Kalpana, Trivedi, Jalpa, Jaiswal, Varun, Kanwar, Shamsher S., Pokharel, Yuba Raj
• Format: Article
• Language: English
• Subjects: AFM study; Anti-cancerous; Antimicrobial; Benzothiazole-bioconjugates; Glucosamine
• ISSN: 2365-6549; 2365-6549
• DOI: 10.1002/slct.201801936

Micro‐organism resistance to the drugs has made it necessary to explore novel antibacterial drugs that have significant toxicities. Herein, we report the bioconjugates of N‐acetyl‐D‐glucosamine with benzothiazole derivatives via ester linkage, which display potent effect against pathogenic micro‐organisms (E. coli, S. aureus and C. albicans). These newly synthesized compounds have also been evaluated for anticancer (Hep‐2 and caco cell lines) and antioxidant activities. The results supported that bioconjugates suppress pathogenic infections (in‐vitro) more effectively in comparison to equivalent dosage of non‐conjugated benzothiazole. Specifically, bioconjugates of Schiff derivative of methoxy‐benzothiazol (compound 8) and nitro‐ benzothiazole (compound 9) showed MIC value of 1.25 μg/mL against C. albicans. The above proved potent compound 9, furthermore, revealed significant activity against Hep‐2 and caco cell lines. In conclusion, this study proved that integration of biocomponent enhances the competence in biological application and the results can be explored as a lead for further improvization for commercialization. The benzothiazole‐bioconjugates with glucosamine showed the preferential results in biological activities due to enhanced interactions as evident in AFM results in comparison to its analogues.