Chloroacetamide derivatives as a promising topical treatment for fungal skin infections. (4th July 2019)

• Record Type: Journal Article
• Authors: Machado, Gabriella da Rosa Monte; Fernandes de Andrade, Saulo; Pippi, Bruna; Bergamo, Vanessa Zafaneli; Jacobus Berlitz, Simone; Lopes, William; Lavorato, Stefânia Neiva; Clemes Külkamp Guerreiro, Irene; Vainstein, Marilene Henning; Teixeira, Mário Lettieri; Alves, Ricardo José; Fuentefria, Alexandre Meneghello
• Is Part Of: Mycologia. Volume 111:Number 4(2019)
• Page Start: 612
• Page End: 623
• Publication Date: 2019-07-04
• Subjects: Candida spp -- chloroacetamide derivatives -- dermatophyte -- film-forming system -- fungal infections -- new chemical entities; Mycology -- Periodicals; Mycologie -- Périodiques; Mycology; Electronic journals; Periodicals; 579.505
• DOI: 10.1080/00275514.2019.1620550
• Languages: English
• ISSNs: 0027-5514

Abstract

ABSTRACT: The aim of this study was to evaluate the antifungal potential of 11 chloroacetamide derivatives and derivative incorporated into a film-forming system (FFS) as a potential alternative for the topical treatment of superficial and skin mycoses. The minimum inhibitory concentration (MIC) evaluation followed Clinical and Laboratory Standards Institute protocols M27-A3 ( Candida ) and M28-A2 (dermatophytes). Compounds2, 3, and4 were the most effective against Candida species (MIC range: 25–50 µg/mL) and dermatophytes (MIC range: 3.12–50 µg/mL). Compound2 maintained its antifungal activity when incorporated in a FFS, with MIC values equivalent to the free compound. In addition, the compound does not act through complexation with ergosterol, suggesting that it may act on other targets of the fungal cell membrane. Chloroacetamide derivatives presented anti- Candida and anti-dermatophytic effectiveness. The FFS containing compound2 has shown to be superior to traditional topical treatment of superficial and cutaneous fungal infections. It was found that these new chemical entities, with their applicability, are an excellent alternative to the topical treatment of fungal skin infections.