Abstract
Arylsulfonamides bearing (aza)norbornane and related motifs were evaluated for: (1) antimicrobial activity toward five key ESKAPE pathogenic bacteria, one Gram‐positive bacteria methicillin‐resistant Staphylococcus aureus (MRSA, ATCC 43300), four Gram‐negative bacteria, Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Acinetobacter baumannii (ATCC 19606), and Pseudomonas aeruginosa (ATCC 27853), and (2) antifungal activity towards two pathogenic fungal strains - Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (H99; ATCC 208821). Four compounds with 4-nitrobenzenesulfonamide motif (VP-4556, VP-4604, VP-4605, and VP-4509) demonstrated high toxicity towards methicillin‐resistant Staphylococcus aureus (ATCC 43300) with the MIC value of 14.7–49.3 µM. These compounds also possessed high antibacterial activity towards gram-negative bacteria P. aeruginosa (ATCC9027) with the MIC value of 460–555 µM. According to the results of toxicity studies of the compounds to HEK-293, HaCaT, Balb/c 3T3, red blood cells and normal mitogen-activated lymphocytes, three compounds - VP-4556, VP-4604 and VP-4509 - bearing azanorbornene, octahydro-3,5-methanocyclopenta[b]pyrrole and bio-isosteric piperidine motifs were selected for further studies as biocompatible agents with promising antimicrobial activity.
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