Synthesis and Biological Evaluation of Novel FtsZ-targeted 3-arylalkoxy-2,6-difluorobenzamides as Potential Antimicrobial Agents

被引：10

作者：

Qiang, Shengsheng ^{[1
]}

Wang, Changde ^{[1
]}

Venter, Henrietta ^{[2
]}

Li, Xin ^{[1
]}

Wang, Yi ^{[1
]}

Guo, Liwei ^{[1
]}

Ma, Ruixin ^{[3
]}

Ma, Shutao ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharmaceut Sci, Key Lab Chem Biol, Dept Med Chem,Minist Educ, 44 West Culture Rd, Jinan 250012, Peoples R China

[2] Univ S Australia, Sansom Inst Hlth Res, Sch Pharm & Med Sci, GPO Box 2471, Adelaide, SA 5001, Australia

[3] Qingdao Univ, Coll Med, Affiliated Hosp, Qingdao 266003, Peoples R China

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2016年 / 87卷 / 02期

基金：

中国国家自然科学基金;

关键词：

2,6-difluorobenzamide; antibacterial activity; FtsZ inhibitors; on-target activity; synthesis; BACTERIAL-CELL-DIVISION; PROTEIN FTSZ; ANTIBACTERIAL ACTIVITY; STAPHYLOCOCCUS-AUREUS; INHIBITORS; DERIVATIVES;

D O I：

10.1111/cbdd.12658

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu g/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 mu g/mL) against Staphylococcus aureus ATCC25923.

引用

页码：257 / 264

页数：8