2. Academic Validation
  3. Preventing Candida albicans biofilm formation using aromatic-rich piperazines

Preventing Candida albicans biofilm formation using aromatic-rich piperazines

  • Bioorg Med Chem. 2020 Dec 1;28(23):115810. doi: 10.1016/j.bmc.2020.115810.
Gaëlle Simon 1,  Christopher Bérubé 2,  Pierre-Alexandre Paquet-Côté 2,  Daniel Grenier 3,  Normand Voyer 4
Affiliations

Affiliations

  • 1 Département de Chimie and PROTEO, Université Laval, 1045 Avenue de la Médecine, Québec, QC G1V 0A6, Canada; Groupe de Recherche en Écologie Buccale, Faculté de Médecine Dentaire, Université Laval, 2420 Rue de la Terrasse, Québec, QC G1V 0A6, Canada.
  • 2 Département de Chimie and PROTEO, Université Laval, 1045 Avenue de la Médecine, Québec, QC G1V 0A6, Canada.
  • 3 Groupe de Recherche en Écologie Buccale, Faculté de Médecine Dentaire, Université Laval, 2420 Rue de la Terrasse, Québec, QC G1V 0A6, Canada.
  • 4 Département de Chimie and PROTEO, Université Laval, 1045 Avenue de la Médecine, Québec, QC G1V 0A6, Canada. Electronic address: normand.voyer@chm.ulaval.ca.
PMID: 33091849 DOI: 10.1016/j.bmc.2020.115810
Abstract

The global increase in microbial resistance is an imminent threat to public health. Effective treatment of infectious diseases now requires new antimicrobial therapies. We report herein the discovery of aromatic-rich piperazines that inhibit biofilm formation by C. albicans. 22 piperazines, including 16 novel ones, were prepared efficiently using a combination of solid- and solution phase synthesis. The most potent compound prevents morphological switching under several hypha-inducing conditions and reduces C. albicans' ability to adhere to epithelial cells. These processes are essential to the development of Candida biofilms, which are associated with its increased resistance to immune defenses and Antifungal agents.

Keywords

Antibiofilm; Candida albicans; Morphological switching; Oxime resin; Piperazines.

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