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Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey





Abstract In this study, 5-pyrimidin-2-ylthiomethyl-1,3,4-oxadiazole-23H-thione 3 was synthesized via the ring closure reaction of 2-pyrimidin-2-ylthioacetohydrazide 2 with carbon disulphide. New oxadiazole derivatives 4a-f were obtained by the nucleophilic substitution reaction of compound 3 with various phenacyl bromides. The chemical structures of the compounds were elucidated by IR, 1H-NMR, 13C-NMR and FAB+-MS spectral data and elemental analyses. The newly synthesized derivatives 4a-f were tested in vitro by using a microbroth dilution method against C. albicans clinical isolate, Osmangazi University, Faculty of Medicine, Eskişehir, Turkey, C. albicans ATCC 90028, C. glabrata clinical isolate, Osmangazi University, Faculty of Medicine, Eskişehir, Turkey, C. tropicalis NRRL Y-12968, C. krusei NRRL Y-7179, C. parapsilosis NRRL Y- 12696, C. albicans NRRL Y-12983, C. glabrata clinical isolate, Anadolu University, Faculty of Science, Department of Biology, Eskişehir, Turkey. Among these compounds, compound 4a was found to be the most potent derivative MIC = 0.007–0.06 versus ketoconazole: 0.001–0.007 mg-mL against Candida species, except C. tropicalis and C. krusei when compared with the standard antifungal ketoconazole.

Keywords: oxadiazole; pyrimidine; anticandidal activity oxadiazole; pyrimidine; anticandidal activity





Autor: Zafer Asim Kaplancikli

Fuente: http://mdpi.com/



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