吡啶基杂环肼:具有高效抗菌活性的跨膜 H+/Cl- Symporters。

IF 3.8 2区 医学 Q2 CHEMISTRY, MEDICINAL
Abhishek Mondal, Manisha Siwach, Manzoor Ahmad, Sunish Kumar Radhakrishnan and Pinaki Talukdar*, 
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引用次数: 0

摘要

随着细菌不断进化并对抗生素产生抗药性,开发强效抗菌剂变得越来越困难。因此,当务之急是找到有效的抗菌剂,以应对传染病和抗生素耐药性带来的不断变化的挑战。使用人工跨膜离子转运体是解决这一问题的一个新兴且前景广阔的途径。我们报告了作为高效跨膜盐酸合剂的吡啶连接杂酰肼。这些化合物通过合作质子化作用提供了一个适当的盐酸结合位点,然后识别氯离子。这些化合物通过影响细胞包膜的平衡,抑制不同革兰氏阴性细菌菌株的生长,效果显著。这一类特殊的化合物在不断开发高效抗菌剂的过程中大有可为。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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

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

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

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.

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来源期刊
ACS Infectious Diseases
ACS Infectious Diseases CHEMISTRY, MEDICINALINFECTIOUS DISEASES&nb-INFECTIOUS DISEASES
CiteScore
9.70
自引率
3.80%
发文量
213
期刊介绍: ACS Infectious Diseases will be the first journal to highlight chemistry and its role in this multidisciplinary and collaborative research area. The journal will cover a diverse array of topics including, but not limited to: * Discovery and development of new antimicrobial agents — identified through target- or phenotypic-based approaches as well as compounds that induce synergy with antimicrobials. * Characterization and validation of drug target or pathways — use of single target and genome-wide knockdown and knockouts, biochemical studies, structural biology, new technologies to facilitate characterization and prioritization of potential drug targets. * Mechanism of drug resistance — fundamental research that advances our understanding of resistance; strategies to prevent resistance. * Mechanisms of action — use of genetic, metabolomic, and activity- and affinity-based protein profiling to elucidate the mechanism of action of clinical and experimental antimicrobial agents. * Host-pathogen interactions — tools for studying host-pathogen interactions, cellular biochemistry of hosts and pathogens, and molecular interactions of pathogens with host microbiota. * Small molecule vaccine adjuvants for infectious disease. * Viral and bacterial biochemistry and molecular biology.
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