Synthesis and biological evaluation of novel FtsZ-targeted 3-arylalkoxy-2,6-difluorobenzamides as potential antimicrobial agents
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Date
2016
Authors
Qiang, S.
Wang, C.
Venter, H.
Li, X.
Wang, Y.
Guo, L.
Ma, R.
Ma, S.
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Journal article
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Chemical Biology and Drug Design, 2016; 87(2):257-264
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Abstract
Novel series of 3-O-arylalkylbenzamide and 3-O-arylalkyl-2,6-difluorobenzamide derivatives were synthesized and evaluated for their on-target activity and antibacterial activity. The results indicated that the 3-O-arylalkyl-2,6-difluorobenzamide derivatives possessed much better on-target activity and antibacterial activity than the 3-O-arylalkylbenzamide derivatives. Among them, 3-O-chlorobenzyl derivative 36 was the most effective in antibacterial activity (0.5, 4, and 8 μg/mL) against Bacillus subtilis ATCC9372, methicillin-resistant Staphylococcus aureus ATCC29213, and penicillin-resistant Staphylococcus aureus PR, while 3-O-methylbenzyl derivative 41 only exhibited the most potent activity (2 μg/mL) against Staphylococcus aureus ATCC25923. 3-O-Chlorobenzyl and 3-O-methylbenzyl derivatives 36 and 41 exhibited the most potent cell division inhibitory activity and antibacterial activity against four phenotypes of Gram-positive strains including MRSA.
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Copyright 2015 John Wiley & Sons
Access Condition Notes: Postprint available on Open access