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synthesis of some oxadiazole derivatives as new anticandidal agents合成一些oxadiazole衍生品新anticandidal代理.pdf

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synthesis of some oxadiazole derivatives as new anticandidal agents合成一些oxadiazole衍生品新anticandidal代理

Molecules 2011, 16, 7662-7671; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis of Some Oxadiazole Derivatives as New Anticandidal Agents Zafer Asim Kaplancikli Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey; E-Mail: zakaplan@.tr; Tel.: +90-222-3350580/3776; Fax: +90-222-3350750 Received: 25 July 2011; in revised form: 23 August 2011 / Accepted: 6 September 2011 / Published: 7 September 2011 Abstract: In this study, 5-[(pyrimidin-2-ylthio)methyl]-1,3,4-oxadiazole-2(3H)-thione (3) was synthesized via the ring closure reaction of 2-(pyrimidin-2-ylthio)acetohydrazide (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 1 13 + structures of the compounds were elucidated by IR, H-NMR, C-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. g