Novel benzenesulfonamide bearing 1,2,4-triazoles as potent anti-microbial and anti-oxidant agents

MEDICINAL CHEMISTRY RESEARCH(2023)

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摘要
A series comprising 30 novel benzenesulfonamide bearing 1,2,4-triazoles 1a – 1h , 2a – 2h , 3a – 3h , 4b – 4f and 4h has been synthesized and investigated as anti-microbial and anti-oxidant agents. All the tested compounds exhibited moderate to excellent inhibitory potential against tested Gram-positive ( Staphylococcus aureus ATCC 6538P, Listeria monocytogenes MTCC 657 , and Bacillus cereus ATCC 11770) and Gram-negative ( Pseudomonas aeruginosa ATCC 15442, Escherichia coli MTCC 143, Salmonella typhi MTCC 733, Shigella flexneri ATCC 9199 ) bacterial strains with minimum inhibitory concentration values ranging from 3.12 to 12.5 µg/mL. Compound 3d was either equipotent or better inhibitor than reference drugs against all tested bacterial as well as fungal strains. All the tested compounds were also found to be safe to normal cells with 89.8–99.8% cell viability against mouse fibroblast cell line and 100% safe to plant seed germination. Final compounds were also screened for their anti-oxidant profile using DPPH method and compound 4d was found to possess highest anti-oxidant acitivity (94.35%). Graphical Abstract
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关键词
1,2,4-Triazole,Benzenesulfonamide,Anti-microbial,Activity,Anti-oxidant,Structure-activity relationship
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