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New antibacterial-core structures based on styryl quinolinium.

Eunsuk Kim1, Seung-Heon Lee1, Seung-Jun Lee1

  • 11Department of Molecular Science and Technology, Ajou University, Suwon, Gyeonggi, 16499 Korea.

Food Science and Biotechnology
|September 29, 2018
PubMed
Summary

New quinolinium salts show potent antimicrobial activity against Gram-positive and Gram-negative bacteria. Electron-withdrawing groups enhance efficacy, and synergistic effects were observed when combined with ampicillin.

Keywords:
bacteriapathogenquinoliniumresistancesusceptibility

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Area of Science:

  • Medicinal Chemistry
  • Antimicrobial Agents
  • Organic Synthesis

Background:

  • Quaternary quinolinium salts are explored as alternative antimicrobial agents.
  • Improving existing quinolinium compounds is crucial for enhanced efficacy.
  • Understanding structure-activity relationships guides the development of novel antimicrobials.

Purpose of the Study:

  • To design and synthesize novel styryl quinolinium derivatives.
  • To evaluate the antibacterial activity of these derivatives against Gram-positive and Gram-negative bacteria.
  • To investigate the relationship between chemical structure and antimicrobial potency.

Main Methods:

  • Rational design of 10 styryl quinolinium derivatives with varied substituents.
  • Determination of minimum inhibitory concentrations (MICs) for antibacterial activity.
  • Assessment of synergistic effects with ampicillin.

Main Results:

  • Six compounds demonstrated bactericidal effects against Gram-positive bacteria (MICs: 2.4–37.5 μg/mL).
  • Two compounds showed activity against Gram-negative bacteria (MICs: 18.75–75 μg/mL).
  • Compounds with strong electron-withdrawing groups exhibited superior activity.

Conclusions:

  • The study provides a foundation for developing potent quinolinium-based antimicrobials.
  • Electron-withdrawing substituents are key for enhancing antibacterial activity.
  • Synergistic antimicrobial effects were observed with ampicillin co-administration.