Antifungal activity and mechanism of action of 2-chloro-N -phenylacetamide: a new molecule with activity against strains of Aspergillus flavus
| Autor: | Edeltrudes de Oliveira Lima, José Maria Barbosa-Filho, Elba Dos Santos Ferreira, Daniele de Figueredo Silva, Luciana Scotti, Ricardo Dias de Castro, Laísa Vilar Cordeiro, Helivaldo Diógenes da Silva Souza, Petrônio Filgueiras de Athayde-Filho |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Antifungal Agents
2-chloro-N-phenylacetamide Science Aspergillus flavus Microbial Sensitivity Tests Microbiology resistance Minimum inhibitory concentration chemistry.chemical_compound Amphotericin B medicine Voriconazole chemistry.chemical_classification Aspergillus Ergosterol Multidisciplinary biology Chemistry antifungal activity Triazoles biology.organism_classification Molecular Docking Simulation Mechanism of action Azole medicine.symptom medicine.drug |
| Zdroj: | Anais da Academia Brasileira de Ciências, Vol 93, Iss suppl 3 (2021) Anais da Academia Brasileira de Ciências v.93 suppl.3 2021 Anais da Academia Brasileira de Ciências Academia Brasileira de Ciências (ABC) instacron:ABC Anais da Academia Brasileira de Ciências, Volume: 93 Supplement 3, Article number: e20200997, Published: 20 SEP 2021 |
| ISSN: | 1678-2690 |
| Popis: | Aspergillus genus causes many diseases, and the species Aspergillus flavus is highly virulent. Treatment of aspergillosis involves azole derivatives such as voriconazole and polyenes such as amphotericin B. Due to an increase in fungal resistance, treatments are now less effective; the search for new compounds with promising antifungal activity has gained importance. The aims of this study were to evaluate the effects of the synthetic amide 2-chloro-N-phenylacetamide (A1Cl) against strains of Aspergillus flavus and to elucidate its mechanism of action. Thus, the minimum inhibitory concentration, minimum fungicidal concentration, conidial germination, associations with antifungal agents, cell wall activities, membrane activities and molecular docking were evaluated. A1Cl presented antifungal activity against Aspergillus flavus strains with a minimum inhibitory concentration of between 16 and 256 μg/mL and a minimum fungicidal concentration between 32 and 512 μg/mL. The minimum inhibitory concentration of A1Cl also inhibited conidial germination, but when associated with amphotericin B and voriconazole, it promoted antagonistic effects. Binding to ergosterol on the fungal plasma membrane is the likely mechanism of action, along with possible inhibition of DNA synthesis through the inhibition of thymidylate synthase. It is concluded that the amide 2-chloro-N-phenylacetamide has promising antifungal potential. |
| Databáze: | OpenAIRE |
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