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Synthesis and Biological Evaluation of Novel FtsZ‐targeted 3‐arylalkoxy‐2,6‐difluorobenzamides as Potential Antimicrobial Agents
Author(s) -
Qiang Shengsheng,
Wang Changde,
Venter Henrietta,
Li Xin,
Wang Yi,
Guo Liwei,
Ma Ruixin,
Ma Shutao
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12658
Subject(s) - staphylococcus aureus , bacillus subtilis , antibacterial activity , antimicrobial , chemistry , derivative (finance) , penicillin , biological activity , ftsz , combinatorial chemistry , microbiology and biotechnology , bacteria , antibiotics , biochemistry , escherichia coli , biology , organic chemistry , in vitro , gene , genetics , financial economics , economics
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 μ g/mL) against Bacillus subtilis ATCC 9372, methicillin‐resistant Staphylococcus aureus ATCC 29213, and penicillin‐resistant Staphylococcus aureus PR , while 3‐ O ‐methylbenzyl derivative 41 only exhibited the most potent activity (2 μ g/mL) against Staphylococcus aureus ATCC 25923.
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