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铜绿假单胞菌PAO1是一种革兰氏阴性机会性人类病原菌,易感染免疫受损的人群.Ⅲ型分泌系统(Type threesecretion system,T3SS)是其主要的致病因子.T3SS抑制剂的策略是抑制铜绿假单胞菌表达及分泌毒力蛋白,阻止其对宿主细胞的侵染.在一种已知T3SS抑制剂的结构基础上,设计和合成了20种α-苯氧基酰胺新衍生物,系统研究了它们的构效关系,研究表明有5种新衍生物对铜绿假单胞菌的一个效应子编码基因exoS的表达具有明显抑制作用.其中N-(2-吡啶基甲基)-2-(2,4-二氯苯氧)-丁酰胺(5r)的活性强于已知的抑制剂MBX1641,并具有很好的水溶性.
Pseudomonas aeruginosa PAO1 is a Gram-negative opportunistic human pathogen, susceptible to immune compromised people. Type III secretion system (Type III secretion system, T3SS) is its main virulence factor.T3SS inhibitor strategy Is to inhibit Pseudomonas aeruginosa expression and secretion of virulence proteins, to prevent its infection of host cells in a known T3SS inhibitor structure based on the design and synthesis of 20 kinds of α-phenoxy amide new derivative Their structure-activity relationship has been systematically studied and the results show that five new derivatives have significant inhibitory effect on the expression of exoS, an effector gene of Pseudomonas aeruginosa. Among them, N- (2-pyridylmethyl) -2- (2,4-dichlorophenoxy) -butyramide (5r) is more active than the known inhibitor MBX1641 and has good water solubility.