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Synthesis and biological evaluation of novel benzyl piperazine derivatives of 5-(5-nitroaryl)-134-thiadiazoles as Anti-Helicobacter pylori agents

机译:新型5-(5-硝基芳基)-134-噻二唑类苄基哌嗪衍生物的合成及生物学评价

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摘要

Background and the purpose of the studyHelicobacter pylori is recognized as the main cause of gastritis and gastroduodenal ulcers and classified as class 1 carcinogen pathogen. Different 1,3,4-thiadiazole derivatives bearing 5-nitroaryl moiety have been shown considerable anti- H. pylori activity. In attempt to find new and potent derivatives of described scaffold, a new series of 1-(substituted benzyl)-4-(5-(5-nitroaryl-2-yl)-1,3,4-thiadiazol-2-yl)piperazine derivatives were synthesized and evaluated against three metronidazole-resistant isolates of H. pylori using paper disk diffusion bioassay test.
机译:研究背景和目的幽门螺杆菌被认为是引起胃炎和十二指肠溃疡的主要原因,被归为1类致癌病原体。具有5-硝基芳基部分的不同的1,3,4-噻二唑衍生物已经显示出相当大的抗幽门螺杆菌活性。为了找到所述支架的新的和有效的衍生物,新系列的1-(取代的苄基)-4-(5-(5-硝基芳基-2-基)-1,3,4-噻二唑-2-基合成哌嗪衍生物,并使用纸盘扩散生物测定测试针对三种耐甲硝唑的幽门螺杆菌菌株进行评估。

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