In:
Bulletin of the Korean Chemical Society, Wiley, Vol. 42, No. 4 ( 2021-04), p. 577-582
Abstract:
Forty‐one fusaric acid analogs possessing a pyridine carboxylic acid scaffold have been synthesized. The antibacterial activity results demonstrated that compounds 5b , 7b , 8c , and 8d displayed strong antibacterial activities against Staphylococcus aureus ATCC25923 with minimum inhibitory concentrations (MICs) of 4–16 μg/mL. Molecular docking study indicated that these compounds have strong hydrogen‐bonding interactions with TyrRS. Meanwhile, 8c and 8d showed promising antibacterial activities against Pseudomonas aeruginosa ATCC9027. Compound 4 exhibited pronounced antibacterial activities against a clinically isolated multidrug‐resistant strain of Escherichia coli (MIC: 64 μg/mL as compared 64 μg/mL of levofloxacin and 1024 μg/mL of ceftriaxone sodium). Moreover, compound 17e displayed strong synergistic antibacterial effect with levofloxacin against the multidrug‐resistant strain, decreasing the MIC value of levofloxacin to 1/16 of its original MIC. No obvious cytotoxic activities against LO2 was observed for compounds 4 , 5b , 8c , 8d , 17d , and 17e at 50 μM. The preliminary structure–activity relationship of fusaric acid analogs was also discussed.
Type of Medium:
Online Resource
ISSN:
1229-5949
,
1229-5949
Language:
English
Publisher:
Wiley
Publication Date:
2021
detail.hit.zdb_id:
2056474-0
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