ArticlePharmaceuticals (Basel, Switzerland)2022
New Membrane Active Antibacterial and Antiviral Amphiphiles Derived from Heterocyclic Backbone of Pyridinium-4-Aldoxime.
Article in Pharmaceuticals (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed.
- Development of Naphthalene-Derivative Bis-QACs as Potent Antimicrobials: Unraveling Structure-Activity Relationship and Microbiological Properties.Molecules (Basel, Switzerland) · 2024Article
- Further Study of the Polar Group's Influence on the Antibacterial Activity of the 3-Substituted Quinuclidine Salts with Long Alkyl Chains.Antibiotics (Basel, Switzerland) · 2023Article
- Synthesis and Biological Evaluation of 3-Amidoquinuclidine Quaternary Ammonium Compounds as New Soft Antibacterial Agents.Pharmaceuticals (Basel, Switzerland) · 2023Article
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Authors and funding
9 authors.
Funding
Abstract
Quaternary ammonium salts (QAS) are irreplaceable membrane-active antimicrobial agents that have been widely used for nearly a century. Cetylpyridinium chloride (CPC) is one of the most potent QAS. However, recent data from the literature indicate that CPC activity against resistant bacterial strains is decreasing. The major QAS resistance pathway involves the QacR dimer, which regulates efflux pump expression. A plausible approach to address this issue is to structurally modify the CPC structure by adding other biologically active functional groups. Here, a series of QAS based on pyridine-4-aldoxime were synthesized, characterized, and tested for antimicrobial activity in vitro. Although we obtained several potent antiviral candidates, these candidates had lower antibacterial activity than CPC and were not toxic to human cell lines. We found that the addition of an oxime group to the pyridine backbone resulted in derivatives with large topological polar surfaces and with unfavorable cLog
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