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Synthesis and antifungal activity of novel oxazolidin-2-one linked-1,2,3-triazole derivatives
ArtĂculo IndizadoNovel oxazolidin-2-one-linked 1,2,3-triazole derivatives (4aâk) were synthesized by straightforward and versatile azideâenolate (3 + 2) cycloaddition. The series of compounds was screened for antifungal activity against four filamentous fungi as well as six yeast species of Candida spp. According to their efficiency and breadth of scope, they can be ordered as 4k > 4d > 4h > 4a, especially in relation to the activity displayed against Candida glabrata ATCC-34138, Trichosporon cutaneum ATCC-28592 and Mucor hiemalis ATCC-8690, i.e. compounds 4d, 4h and 4k showed excellent activity against C. glabrata (MIC 0.12, 0.25 and 0.12 ÎŒg mLâ1, respectively), better than that of itraconazole (MIC 1 ÎŒg mlâ1). The activity of compound 4d (MIC = 2 ÎŒg mLâ 1) was higher than that observed for the standard antifungal drug (MIC = 8 ÎŒg mLâ1) against Trichosporon cutaneum, while compound 4k displayed an excellent antimycotic activity against Mucor hiemalis (MIC = 2 ÎŒg mLâ1 vs. 4 ÎŒg mLâ1 for itraconazole). In addition, we describe herein a novel mild and eco-friendly synthetic protocol for obtaining ÎČ-ketosulfones (adducts to afford compounds 4aâk) from α-brominated carbonyls in an aqueous nanomicellar medium at room temperature.CONACYT, SecretarĂa de InvestigaciĂłn de Estudios Avanzados de la UAE