Antimicrobial action of arylsulfonamides bearing (aza)norbornane and related motifs: evaluation of new promising anti-MRSA agents
نویسندگان
چکیده
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 Escherichia coli (ATCC 25922), Klebsiella pneumonia 700603), Acinetobacter baumannii 19606), Pseudomonas aeruginosa 27853), (2) antifungal towards two fungal strains - Candida albicans 90028) Cryptococcus neoformans var. Grubii (H99; 208821). Four compounds with 4-nitrobenzenesulfonamide motif (VP-4556, VP-4604, VP-4605, VP-4509) demonstrated high toxicity 43300) the MIC value of 14.7–49.3 µM. These also possessed antibacterial gram-negative P. (ATCC9027) 460–555 According to results studies HEK-293, HaCaT, Balb/c 3T3, red blood cells normal mitogen-activated lymphocytes, three VP-4556, VP-4604 VP-4509 azanorbornene, octahydro-3,5-methanocyclopenta[b]pyrrole bio-isosteric piperidine selected for further as biocompatible agents promising activity.
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ژورنال
عنوان ژورنال: Medicinal Chemistry Research
سال: 2022
ISSN: ['1554-8120', '1054-2523']
DOI: https://doi.org/10.1007/s00044-021-02827-1