Synthesis, characterization and biological screening of pyrazole-conjugated benzothiazole analogs

Mahesh Bhat and Shiddappa, L. B. (2018) Synthesis, characterization and biological screening of pyrazole-conjugated benzothiazole analogs. Future Medicinal Chemistry, 10 (1). pp. 71-87. ISSN 1756-8927

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Aim: Benzothiazole and pyrazoles are two important pharmacophores, the activity can be enhanced by conjugating them. Here, two novel series of the pyrazole-conjugated benzothiazole derivatives were synthesized. Results: Synthesized compounds were characterized by Fourier-transform infrared, LC-MS, 1H NMR and 13C NMR spectroscopic techniques. Synthesized compounds exhibited moderate antimicrobial, antioxidant and excellent anti-TB activities. In in vitro anti-TB activity, 4d and 4e exhibited 1.6 μg/ml minimum inhibitory concentration value. In order to rationalize the anti-TB activity, molecular docking studies were carried out and they were correlated with the in vitro results. Conclusion: Compounds containing electron donating groups show the promising antimicrobial and antioxidant activities, compounds with CH3 and Cl substitution show excellent anti-TB activity. Synthesized molecules may become potential candidates for the clinical trials.

Item Type: Article
Subjects: B Life Science > Environmental Science
Divisions: Department of > Environmental Science
Depositing User: manjula User
Date Deposited: 17 Jul 2019 06:18
Last Modified: 17 Jul 2019 06:18

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