Sorbonne University, Université de technologie de Compiègne, ESCOM, EA TIMR 4297, Centre de recherche de Royallieu, CS 60319, 60203 Compiègne Cedex, France.
TERRA Research Center, Laboratory of Molecular Biophysics at Interfaces, SFR Condorcet, Gembloux Agro-Bio Tech, University of Liege, Passage des Déportés, 2, 5030 Gembloux, Belgium.
Bioorg Chem. 2020 Jan;94:103399. doi: 10.1016/j.bioorg.2019.103399. Epub 2019 Oct 28.
With the emergence of multi-drug resistant bacteria and hospital-acquired infections, there is an urgent need to develop new antibiotics. Here, we report the synthesis, physico-chemical characterizations, and antimicrobial activity assays of four Azo compounds that differ in their alkyl chain length. The molecular mechanism of their antibacterial activity was investigated by complementary in vitro and in silico biophysical studies. The compounds with alkyl chain lengths of four or six carbons showed a low MIC against Escherichia coli and Bacillus subtilis. Our investigations into the mechanism of their action revealed that phosphatidylethanolamine in the bacterial plasma membrane plays an important role in their antibacterial activity.
随着多药耐药菌和医院获得性感染的出现，迫切需要开发新的抗生素。在这里，我们报告了四种偶氮化合物的合成、物理化学特性和抗菌活性测定，它们在烷基链长度上有所不同。通过体外和计算机辅助的生物物理研究，我们研究了它们的抗菌活性的分子机制。具有四个或六个碳原子烷基链长度的化合物对大肠杆菌和枯草芽孢杆菌的 MIC 值较低。我们对其作用机制的研究表明，细菌质膜中的磷脂酰乙醇胺在其抗菌活性中起着重要作用。
