Study of Benzofuroquinolinium Derivatives as a New Class of Potent Antibacterial Agent and the Mode of Inhibition Targeting FtsZ.
Study of Benzofuroquinolinium Derivatives as a New Class of Potent Antibacterial Agent and the Mode of Inhibition Targeting FtsZ.
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新型强效抗菌剂苯并呋喹啉衍生物及其针对 FtsZ 的抑制模式研究
DOI：
10.3389/fmicb.2018.01937
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发表时间：
2018
影响因子：
5.2
通讯作者：
Wong KY
中科院分区：
文献类型：
--
作者：
Zheng YY;Du RL;Cai SY;Liu ZH;Fang ZY;Liu T;So LY;Lu YJ;Sun N;Wong KY
为了对抗多重耐药菌的出现，迫切需要新一代抗菌药物。FtsZ目前被确定为新型抗菌化合物开发的一个有前途的目标，因为它的保守特性和它在细菌细胞分裂中发挥的重要作用。本文研究了一系列苯并呋喃并喹啉衍生物的抗菌活性。结果表明，这些化合物对耐药病原体包括MRSA、VREF和NDM-1大肠杆菌具有有效的抗菌活性。生物学研究表明，该化合物是一种有效的抑制剂，能够抑制FtsZ聚合和GT3活性，从而停止细胞分裂并导致细胞死亡。更重要的是，这一系列化合物显示出对哺乳动物细胞的低细胞毒性，因此它们可能成为开发靶向细胞分裂蛋白FtsZ的新抗菌剂的新化学型。
New generation of antibacterial agents are urgently needed in order to fight the emergence of multidrug-resistant bacteria. FtsZ is currently identified as a promising target for new types of antimicrobial compounds development because of its conservative characteristics and its essential role played in bacterial cell division. In the present study, the antibacterial activity of a series of benzofuroquinolinium derivatives was investigated. The results show that the compounds possess potent antibacterial activity against drug resistant pathogens including MRSA, VREF and NDM-1 Escherichia coli. Biological studies reveal that the compound is an effective inhibitor that is able to suppress FtsZ polymerization and GTPase activity and thus stopping the cell division and causing cell death. More importantly, this series of compounds shows low cytotoxicity on mammalian cells and therefore they could be new chemotypes for the development of new antibacterial agents targeting the cell-division protein FtsZ.
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影响因子：
5.2
作者：
Lin J;Nishino K;Roberts MC;Tolmasky M;Aminov RI;Zhang L
通讯作者：
Zhang L
影响因子：
4.1
作者：
Chan KF;Sun N;Yan SC;Wong ILK;Lui HK;Cheung KC;Yuan J;Chan FY;Zheng Z;Chan EWC;Chen S;Leung YC;Chan TH;Wong KY
通讯作者：
Wong KY
影响因子：
5.6
作者：
Chan, Fung-Yi;Sun, Ning;Wong, Kwok-Yin
通讯作者：
Wong, Kwok-Yin
DOI：
10.1126/science.1176667
发表时间：
2009-08-28
期刊：
Science (New York, N.Y.)
影响因子：
--
作者：
Fischbach MA;Walsh CT
通讯作者：
Walsh CT
影响因子：
4.8
作者：
Andreu, Jose M.;Schaffner-Barbero, Claudia;Martin-Galiano, Antonio J.
通讯作者：
Martin-Galiano, Antonio J.