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Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives

2018; Elsevier BV; Volume: 151; Linguagem: Inglês

10.1016/j.ejmech.2018.03.083

1768-3254

Cleudiomar Inácio Lino, Igor Gonçalves de Souza, Beatriz M. Borelli, Thelma Tirone Silvério Matos, Iasmin Natália Santos Teixeira, Jonas Pereira Ramos, Elaine M. Souza–Fagundes, Philipe Oliveira Fernandes, Vinícius Gonçalves Maltarollo, Susana Johann, Renata Barbosa de Oliveira,

Nail Diseases and Treatments

In the search for new antifungal agents, a novel series of fifteen hydrazine-thiazole derivatives was synthesized and assayed in vitro against six clinically important Candida and Cryptococcus species and Paracoccidioides brasiliensis. Eight compounds showed promising antifungal activity with minimum inhibitory concentration (MIC) values ranging from 0.45 to 31.2 μM, some of them being equally or more active than the drug fluconazole and amphotericin B. Active compounds were additionally tested for toxicity against human embryonic kidney (HEK-293) cells and none of them exhibited significant cytotoxicity, indicating high selectivity. Molecular modeling studies results corroborated experimental SAR results, suggesting their use in the design of new antifungal agents.