4.6 Article

Benzothiazole-tethered 1,2,3-triazoles: Synthesis, antimicrobial, antioxidant, and molecular docking studies

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JOURNAL OF MOLECULAR STRUCTURE
卷 1266, 期 -, 页码 -

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ELSEVIER
DOI: 10.1016/j.molstruc.2022.133417

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Benzothiazole; 3-triazole; Antimicrobial; Antioxidant; Molecular docking

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A new series of benzothiazole-1,2,3-triazole compounds were synthesized and tested for their antibacterial and antifungal activities. One derivative showed high antibacterial activity against Escherichia coli, most compounds exhibited remarkable inhibitory effects against Pseudomonas aeruginosa, while another derivative displayed high activity against Candida albicans. Several derivatives also showed high antioxidant activity.
Over the past decades, antibiotic resistance has garnered considerable attention as a public health concern. Therefore, it has become necessary to develop new generations of antibacterial drugs. Here we describe the synthesis of novel benzothiazole-1,2,3-triazoles 12 -21 utilizing copper(I) catalyzed alkyneazide cycloaddition reactions. Compounds 12 -21 were tested for their in vitro antibacterial activity on Gram-positive and Gram-negative bacteria. Derivative 18 displayed high antibacterial activity against Escherichia coli . All compounds exhibited remarkable inhibitory effects against Pseudomonas aeruginosa , except for derivatives 17 and 18 . Antifungal evaluation of compounds 12 -21 revealed high activity of derivative 20 against Candida albicans . Among all the tested compounds, derivatives 17 , 18 , and 19 showed high antioxidant activity . Molecular docking studies were undertaken to validate the antibacterial results. (c) 2022 Published by Elsevier B.V.

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