351444-21-8Relevant articles and documents
Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives
Lino, Cleudiomar Inácio,Gon?alves de Souza, Igor,Santos Teixeira, Iasmin Natália,Maltarollo, Vinícius Gon?alves,de Oliveira, Renata Barbosa,Borelli, Beatriz Martins,Silvério Matos, Thelma Tirone,Johann, Susana,Ramos, Jonas Pereira,Maria de Souza Fagundes, Elaine,de Oliveira Fernandes, Philipe
, p. 248 - 260 (2018)
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.
