Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (06): 1309-1318.DOI: 10.6023/cjoc201302021 Previous Articles     Next Articles



张成芳a, 吴小刚b, 李燕c, 梁翠荣a, 车亦舟b, 顾玲玲a, 任杰a, 胡昆a, 孙小强d, Ching-Hong Yangb, 陈新a   

  1. a 常州大学制药与生命科学学院 常州 213164;
    b Department of Biological Sciences, University of Wisconsin-Milwaukee, Wisconsin 53211, USA;
    c 中国农业大学植物病理系 北京 100193;
    d 常州大学石油化工学院 常州 213164
  • 收稿日期:2013-02-26 修回日期:2013-04-01 发布日期:2013-04-08
  • 通讯作者: 陈新, Ching-Hong Yang;
  • 基金资助:


Synthesis and Bioactivity of Novel Inhibitors for Type III Secretion System of Pseudomonas aeruginosa PAO1

Zhang Chengfanga, Wu Xiaogangb, Li Yanc, Liang Cuironga, Che Yizhoub, Gu Linglinga, Ren Jiea, Hu Kuna, Sun Xiaoqiangd, Yang Ching-Hongb, Chen Xina   

  1. a School of Pharmaceutical and Life Science, Changzhou University, Changzhou 213164;
    b Department of Biological Sciences, University of Wisconsin-Milwaukee, Wisconsin 53211, USA;
    c Department of Plant Disease, China Agricultural University, Beijing 100193;
    d School of Petrochemical Engineering, Changzhou University, Changzhou 213164
  • Received:2013-02-26 Revised:2013-04-01 Published:2013-04-08
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.21272029) and the "333 High-level talent training program" of Jiangsu Province.

Pseudomonas aeruginosa PAO1 is a Gram-negative, opportunistic bacterial human pathogen which infects immunocompromised individuals.The bacterium carries a type III secretion system (T3SS) as a major virulence determinant.The strategy of T3SS inhibitors is to prevent the bacterium from injecting effector proteins into the host, and causing a change in the pathophysiology of the host cells.Based on the structure of a known T3SS inhibitor of P.aeruginosa, 20 new α-phenoxyacetamide derivatives have been designed and synthesized, and the structure-activity relationship results for these new derivatives have been discussed.Five derivatives have shown strong inhibitory effect against exoS gene expression of P.aeruginosa, and among them, N-(2-pyridylmethyl)-2-(2,4-dichlorophenoxy)-butanamide (5r) has not only exhibited stronger potency than the known T3SS inhibitor, but also better solubility in aqueous solution.

Key words: Pseudomonas aeruginosa, type III secretion system, inhibitors, synthesis