A chloroacetamide derivative as a potent candidate for fusariosis treatment

Braz J Microbiol. 2022 Sep;53(3):1289-1295. doi: 10.1007/s42770-022-00771-9. Epub 2022 Jun 1.

Abstract

Fusariosis has presented a significant increase in their incidence in the last years. This epidemiological panorama probably is due to the increasing profile of refractory susceptibility of Fusarium spp. to available drugs, especially in immunocompromised individuals. Thus, the development of new compounds with effectiveness on these organisms is a necessity. This study evaluated the antifungal potential of a chloroacetamide derivative (4-BFCA) against resistant Fusarium strains. As a result, the compound was effective against all strains (MIC range 12.5-50 μg/mL). The time kill assay demonstrated that 4-BFCA presents a concentration-dependent fungicidal action. Although its action mechanism has not yet been elucidated, it was possible to observe its efficacy through damages and alterations provoked along the hyphae of Fusarium spp. 4-BFCA maintained a high survival rate of Tenebrio molitor larvae, suggesting that it does not cause acute systemic toxicity on this host at the concentration evaluated. In addition, 4-BFCA was 83.33% effective in combating a fungal infection in vivo on the chorioallantoid membrane of embryonated eggs. Our results are very promising and arouse interest to investigate the action of 4-BFCA on Fusarium strains since it acts as a possible candidate for the development of new therapies for the treatment of fusariosis.

Keywords: Antifungal resistance; Antifungal therapy; Chloroacetamide derivatives; Fusarium.

MeSH terms

  • Acetamides / pharmacology
  • Acetamides / therapeutic use
  • Antifungal Agents / pharmacology
  • Antifungal Agents / therapeutic use
  • Fusariosis* / drug therapy
  • Fusariosis* / epidemiology
  • Fusariosis* / microbiology
  • Fusarium*
  • Humans

Substances

  • Acetamides
  • Antifungal Agents
  • chloroacetamide