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New thymol-derived triazole exhibits promising activity against Trichophyton rubrum.
de Sousa Cutrim, Thiago Antonio; Eloy, Mariana Alves; Barcelos, Fernando Fontes; Meireles, Leandra Martins; de Freitas Ferreira, Lara Chaves; Reis, Tatiana Alves; Gonçalves, Sarah Santos; Lacerda, Valdemar; Fronza, Marcio; Morais, Pedro Alves Bezerra; Scherer, Rodrigo.
Afiliação
  • de Sousa Cutrim TA; Pharmaceutical Sciences Graduate Program, Universidade Vila Velha, Comissário José Dantas de Melo St., 21, Boa Vista, Vila Velha, Espírito Santo, 29102-770, Brazil.
  • Eloy MA; Agrochemical Graduate Program, Federal University of Espírito Santo, Alegre, Espirito Santo, 29500-000, Brazil.
  • Barcelos FF; Plant Biotechnology Graduate Program, Universidade Vila Velha, Vila Velha, Espírito Santo, 29102-770, Brazil.
  • Meireles LM; Pharmaceutical Sciences Graduate Program, Universidade Vila Velha, Comissário José Dantas de Melo St., 21, Boa Vista, Vila Velha, Espírito Santo, 29102-770, Brazil.
  • de Freitas Ferreira LC; Agrochemical Graduate Program, Federal University of Espírito Santo, Alegre, Espirito Santo, 29500-000, Brazil.
  • Reis TA; Department of Microbiology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, Brazil.
  • Gonçalves SS; Center for Research in Medical Mycology, Department of Pathology, Federal University of Espírito Santo, Vitória, Espírito Santo, Brazil.
  • Lacerda V; Chemistry Graduate Program, Universidade Federal Do Espírito Santo, Vitória, Espírito Santo, Brazil.
  • Fronza M; Pharmaceutical Sciences Graduate Program, Universidade Vila Velha, Comissário José Dantas de Melo St., 21, Boa Vista, Vila Velha, Espírito Santo, 29102-770, Brazil.
  • Morais PAB; Agrochemical Graduate Program, Federal University of Espírito Santo, Alegre, Espirito Santo, 29500-000, Brazil. pedro.morais@ufes.br.
  • Scherer R; Pharmaceutical Sciences Graduate Program, Universidade Vila Velha, Comissário José Dantas de Melo St., 21, Boa Vista, Vila Velha, Espírito Santo, 29102-770, Brazil. rodrigo.scherer@uvv.br.
Braz J Microbiol ; 55(2): 1287-1295, 2024 Jun.
Article em En | MEDLINE | ID: mdl-38453819
ABSTRACT
Fungal infections have emerged worldwide, and azole antifungals are widely used to control these infections. However, the emergence of antifungal resistance has been compromising the effectiveness of these drugs. Therefore, the objective of this study was to evaluate the antifungal and cytotoxic activities of the nine new 1,2,3 triazole compounds derived from thymol that were synthesized through Click chemistry. The binding mode prediction was carried out by docking studies using the crystallographic structure of Lanosterol 14α-demethylase G73E mutant from Saccharomyces cerevisiae. The new compounds showed potent antifungal activity against Trichophyton rubrum but did not show relevant action against Aspergillus fumigatus and Candida albicans. For T. rubrum, molecules nº 5 and 8 showed promising results, emphasizing nº 8, whose fungicidal and fungistatic effects were similar to fluconazole. In addition, molecule nº 8 showed low toxicity for keratinocytes and fibroblasts, concluding that this compound demonstrates promising characteristics for developing a new drug for dermatophytosis caused by T. rubrum, or serves as a structural basis for further research.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Timol / Triazóis / Testes de Sensibilidade Microbiana / Arthrodermataceae / Simulação de Acoplamento Molecular / Antifúngicos Limite: Humans Idioma: En Revista: Braz J Microbiol Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Brasil País de publicação: Brasil
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Timol / Triazóis / Testes de Sensibilidade Microbiana / Arthrodermataceae / Simulação de Acoplamento Molecular / Antifúngicos Limite: Humans Idioma: En Revista: Braz J Microbiol Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Brasil País de publicação: Brasil