2. Academic Validation
  3. Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis

Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis

  • Eur J Med Chem. 2020 Dec 1;207:112821. doi: 10.1016/j.ejmech.2020.112821.
Songuigama Coulibaly 1,  Mena Cimino 2,  Mahama Ouattara 3,  Cédric Lecoutey 4,  Maria V Buchieri 2,  Noelia Alonso-Rodriguez 2,  Julien Briffotaux 5,  Damien Mornico 6,  Brigitte Gicquel 7,  Christophe Rochais 8,  Patrick Dallemagne 9
Affiliations

Affiliations

  • 1 Centre D'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie. Univ, UNICAEN, F-14000, Caen, France; UFR Sciences Pharmaceutiques et Biologiques, Université Félix Houphouët Boigny, Abidjan, Cote d'Ivoire.
  • 2 Unité de Génétique Mycobactérienne, Institut Pasteur, F-75724, Paris, France.
  • 3 UFR Sciences Pharmaceutiques et Biologiques, Université Félix Houphouët Boigny, Abidjan, Cote d'Ivoire.
  • 4 Centre D'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie. Univ, UNICAEN, F-14000, Caen, France.
  • 5 Department of Tuberculosis Control and Prevention, Shenzhen Nanshan Center for Chronic Disease Control, Shenzhen, China.
  • 6 Hub de Bioinformatique et Biostatistique - Département Biologie Computationnelle, Institut Pasteur, USR 3756 CNRS, Paris, France.
  • 7 Unité de Génétique Mycobactérienne, Institut Pasteur, F-75724, Paris, France; Department of Tuberculosis Control and Prevention, Shenzhen Nanshan Center for Chronic Disease Control, Shenzhen, China.
  • 8 Centre D'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie. Univ, UNICAEN, F-14000, Caen, France. Electronic address: christophe.rochais@unicaen.fr.
  • 9 Centre D'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Normandie. Univ, UNICAEN, F-14000, Caen, France. Electronic address: patrick.dallemagne@unicaen.fr.
PMID: 32950907 DOI: 10.1016/j.ejmech.2020.112821
Abstract

Several phenanthrolinic analogs of quinolones have been synthesized and their Antibacterial activity tested against Mycobacterium tuberculosis, other mycobacterial species and bacteria from other genera. Some of them show high activity (of the range observed for rifampicin) against M. tuberculosis replicating in vitro and in vivo (infected macrophages) conditions. These derivatives show the same activity with all or several M. tuberculosis complex Bacterial mutants resistant to fluoroquinolones (FQ). This opens the way to the construction of new drugs for the treatment of FQ resistant Bacterial infections, including tuberculosis. Several compounds showed also activity against Staphylococcus aureus and probably other species. These compounds do not show major toxicity. We conclude that the novel phenanthrolinic derivatives described here are potent hits for further developments of new Antibiotics against Bacterial infectious diseases including tuberculosis in particular those resistant to FQ.

Keywords

Dihydrophenanthrolinones; Fluoroquinolones; Tuberculosis.

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