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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Synthesis and Anti-Helicobacter pylori Acitivity of Pyloricidin Derivatives I. Structure-activity Relationships on the Terminal Peptidic Moiety
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Synthesis and Anti-Helicobacter pylori Acitivity of Pyloricidin Derivatives I. Structure-activity Relationships on the Terminal Peptidic Moiety

机译：Pyloricidin衍生物的合成和抗幽门螺杆菌活性I.末端肽部分的结构活性关系

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摘要

The novel natural antibiotics pyloricidin A, B and C possess potent and highly selective antibacterial activity against Helicobacter pylori. In order to investigate the structure activity relationships for the terminal peptidic moiety, a series of pyloricidin B and pyloricidin C derivatives, bearing various amino acids in the moiety, were prepared and evaluated for their anti-H. pylori activity, The derivaties bearing #alpha#-D-, #beta-and #gamma#-amino acids or peptidemimetics showed drastically decreased activity .On the other hand, the derivatives with #alpha#-L-amino acids were found to maintain the activity . Among the derivatives prepared in this work, the allylglycine derivative 2s showed the most potent anti-H. pylori activity , with an MIC value of less that 0.006 #mu#g/ml against H. pylori NCTC 11637 , which is 60-fold greater than the activity of the lead compound pyloricidin C.
机译：新型天然抗菌素pyloricidin A，B和C对幽门螺杆菌具有有效且高度选择性的抗菌活性。为了研究末端肽部分的结构活性关系，制备了一系列在该部分带有各种氨基酸的吡咯菌素B和吡咯菌素C衍生物，并评估了它们的抗-H。幽门螺杆菌活性，带有＃alpha＃-D-，＃beta-和＃γ＃-氨基酸或肽模拟物的衍生物显示出急剧降低的活性。另一方面，发现带有＃alpha＃-L-氨基酸的衍生物可以维持活动 。在这项工作中制备的衍生物中，烯丙基甘氨酸衍生物2s显示出最有效的抗H物质。幽门螺杆菌活性，针对幽门螺杆菌NCTC 11637的MIC值小于0.006＃mu＃g / ml，比主要化合物幽门螺杆菌C的活性高60倍。

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