Synthesis of Oxadiazole-Thiadiazole Hybrids and Their Anticandidal Activity
AbstractIn the field of infection management, it is a major challenge to discover a potent and safe antifungal agent due to the emergence of resistant strains. Hence, the goal of this paper is to design and synthesize novel oxadiazole-thiadiazole hybrid compounds (6a–6s) and evaluate their antifungal activity. The structures of synthesized compounds were elucidated by various methods including FT-IR, 1H-NMR, 13C-NMR and HR-MS spectral data. Compounds were tested against four Candida species by broth microdilution assay. Compounds 6e, 6k and 6r, bearing a nitro group, showed significant antifungal activity against all fungi with minimum inhibitory concentration (MIC) in the range of 0.78–3.12 µg/mL. These compounds were also screened for their in vitro cytotoxic effects by MTT assay and detected as nontoxic at their active concentrations against Candida strains. To examine the effects of these compounds on ergosterol biosynthesis, the LC-MS-MS method, which is based on quantification of ergosterol level in C. krusei, was carried out. Finally, the most active molecule (6e) was docked in the active site of the lanosterol 14α-demethylase enzyme, and it was determined that there is a strong interaction between the compound and enzyme. View Full-Text
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Levent, S.; Kaya Çavuşoğlu, B.; Sağlık, B.N.; Osmaniye, D.; Acar Çevik, U.; Atlı, Ö.; Özkay, Y.; Kaplancıklı, Z.A. Synthesis of Oxadiazole-Thiadiazole Hybrids and Their Anticandidal Activity. Molecules 2017, 22, 2004.
Levent S, Kaya Çavuşoğlu B, Sağlık BN, Osmaniye D, Acar Çevik U, Atlı Ö, Özkay Y, Kaplancıklı ZA. Synthesis of Oxadiazole-Thiadiazole Hybrids and Their Anticandidal Activity. Molecules. 2017; 22(11):2004.Chicago/Turabian Style
Levent, Serkan; Kaya Çavuşoğlu, Betül; Sağlık, Begüm N.; Osmaniye, Derya; Acar Çevik, Ulviye; Atlı, Özlem; Özkay, Yusuf; Kaplancıklı, Zafer A. 2017. "Synthesis of Oxadiazole-Thiadiazole Hybrids and Their Anticandidal Activity." Molecules 22, no. 11: 2004.
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