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吡啶基连接的杂腙:具有高效抗菌活性的跨膜H⁺/Cl⁻共转运体

Pyridyl-Linked Hetero Hydrazones: Transmembrane H/Cl Symporters with Efficient Antibacterial Activity.

作者信息

Mondal Abhishek, Siwach Manisha, Ahmad Manzoor, Radhakrishnan Sunish Kumar, Talukdar Pinaki

出版信息

ACS Infect Dis. 2024 Feb 9;10(2):371-376. doi: 10.1021/acsinfecdis.3c00455. Epub 2024 Jan 23.

Abstract

The development of potent antibacterial agents has become increasingly difficult as bacteria continue to evolve and develop resistance to antibiotics. It is therefore imperative to find effective antimicrobial agents that can address the evolving challenges posed by infectious diseases and antimicrobial resistance. Using artificial transmembrane ion transporters is an emerging and promising avenue to address this issue. We report pyridyl-linked hetero hydrazones as highly efficient transmembrane HCl symporters. These compounds offer an appropriate HCl binding site through cooperative protonation, followed by recognition of chloride ions. HCl transport by these compounds inhibits the growth of different Gram-negative bacterial strains with high efficacy by affecting the cell envelope homeostasis. This specific class of compounds holds substantial promise in the ongoing pursuit of developing highly efficient antibacterial agents.

摘要

随着细菌不断进化并对抗生素产生耐药性,开发强效抗菌剂变得越来越困难。因此,必须找到有效的抗菌剂,以应对传染病和抗菌药物耐药性带来的不断演变的挑战。使用人工跨膜离子转运体是解决这一问题的一个新兴且有前景的途径。我们报告了吡啶基连接的杂腙作为高效的跨膜HCl同向转运体。这些化合物通过协同质子化提供合适的HCl结合位点,随后识别氯离子。这些化合物介导的HCl转运通过影响细胞膜稳态,高效抑制不同革兰氏阴性菌菌株的生长。在持续追求开发高效抗菌剂的过程中,这类特定的化合物具有很大的前景。

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