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Forward Genetic Approaches in Chlamydia trachomatis
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Modified Fluoroquinolones as Antimicrobial Compounds Targeting Chlamydia trachomatis.

Thi Huyen Vu1, Erika Adhel2, Katarina Vielfort3

  • 1University of Engineering and Technology, Vietnam National University, Hanoi (VNUH), Vietnam.

International Journal of Molecular Sciences
|June 24, 2022
PubMed
Summary

Researchers enhanced fluoroquinolone activity against Chlamydia trachomatis, the leading cause of bacterial sexually transmitted infections and trachoma. Novel molecules show nanomolar activity, offering potential for improved treatments.

Keywords:
8-hydroxyquinolineantibacterialbactericidalinhibitorsiron

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Area of Science:

  • Medicinal Chemistry
  • Antimicrobial Drug Discovery
  • Infectious Diseases

Background:

  • Chlamydia trachomatis is a major cause of bacterial sexually transmitted infections and trachoma, leading to infertility and blindness.
  • Current treatments face challenges, necessitating the development of novel therapeutic strategies.
  • Previous work enhanced fluoroquinolone activity against C. trachomatis via metal chelating moiety grafting.

Purpose of the Study:

  • To further explore pharmacomodulation of fluoroquinolones to enhance antichlamydial activity.
  • To synthesize and evaluate novel molecules with improved efficacy against C. trachomatis.
  • To assess the broader antibacterial spectrum of these novel compounds against other pathogens.

Main Methods:

  • Pharmacomodulation of ciprofloxacin by grafting a metal chelating moiety.
  • Synthesis of novel fluoroquinolone derivatives.
  • Evaluation of antichlamydial activity using EC50 values and testing against Neisseria gonorrhoeae and ESKAPE pathogens.

Main Results:

  • Novel molecules achieved nanomolar activity (EC50) against Chlamydia trachomatis.
  • The enhanced molecules demonstrated selective activity against C. trachomatis.
  • Activity against Neisseria gonorrhoeae and ESKAPE group bacteria was also evaluated.

Conclusions:

  • Pharmacomodulation successfully enhanced the antichlamydial effect of fluoroquinolones.
  • The developed molecules show significant promise for treating C. trachomatis infections.
  • This strategy highlights a viable approach for improving fluoroquinolone-based antimicrobials.