CAGE ARYLSULFONAMIDES AND THEIR ANTIMICROBIAL PROPERTIES
DOI:
https://doi.org/10.15421/jchemtech.v30i1.246451Keywords:
nitrobenzenesulfonamides; (aza)norbornane; 3-azabicyclo[3.2.1]oct-6-ene; cytotoxicity; SwissADME toolAbstract
Arylsulfonamides bearing (aza)norbornane, 3-azabicyclo[3.2.1]oct-6-ene and related motifs were selected and evaluated for antimicrobial activity toward five key ESKAPE pathogenic bacteria, one Gram‐positive bacteria methicillin‐resistant Staphylococcus aureus (ATCC 43300), four Gram‐negative bacteria, Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Acinetobacter baumannii (ATCC 19606), and Pseudomonas aeruginosa (ATCC 27853) and antifungal activity towards two pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (H99; ATCC 208821). One compound with 4-nitrobenzenesulfonamide motif demonstrated high activity towards methicillin‐resistant Staphylococcus aureus (ATCC 43300). The compound VP-4606 has low cytotoxicity towards pseudo-normal cells of HaCaT, Balb/c 3T3 lines, and mitogen-activated lymphocytes isolated from healthy adult peripheral blood of healthy donor up to 2.5 mM.
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