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抗菌环肽类似物的相似性分析、合成与生物测定。

Similarity analysis, synthesis, and bioassay of antibacterial cyclic peptidomimetics.

机构信息

Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA.

出版信息

Beilstein J Org Chem. 2012;8:1146-60. doi: 10.3762/bjoc.8.128. Epub 2012 Jul 24.

Abstract

The chemical similarity of antibacterial cyclic peptides and peptidomimetics was studied in order to identify new promising cyclic scaffolds. A large descriptor space coupled with cluster analysis was employed to digitize known antibacterial structures and to gauge the potential of new peptidomimetic macrocycles, which were conveniently synthesized by acylbenzotriazole methodology. Some of the synthesized compounds were tested against an array of microorganisms and showed antibacterial activity against Bordetella bronchistepica, Micrococcus luteus, and Salmonella typhimurium.

摘要

为了鉴定新的有前途的环状支架,研究了抗菌环肽和类肽的化学相似性。采用了大描述符空间和聚类分析来数字化已知的抗菌结构,并评估新的肽模拟大环的潜力,这些大环可以通过酰基苯并三唑方法方便地合成。一些合成的化合物进行了针对一系列微生物的测试,结果表明它们对支气管博德特氏菌、藤黄微球菌和鼠伤寒沙门氏菌具有抗菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/241b/3458733/6c25a2fdf7ea/Beilstein_J_Org_Chem-08-1146-g002.jpg

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