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Molecules 2019, 24(1), 191; https://doi.org/10.3390/molecules24010191

Synthesis and Antifungal Potential of Some Novel Benzimidazole-1,3,4-Oxadiazole Compounds

1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir 26470, Turkey
2
Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University, Eskişehir 26470, Turkey
3
Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Anadolu University, Eskişehir 26470, Turkey
4
Open Education Faculty, Anadolu University, Eskişehir 26470, Turkey
*
Author to whom correspondence should be addressed.
Academic Editor: Fawaz Aldabbagh
Received: 5 December 2018 / Revised: 24 December 2018 / Accepted: 30 December 2018 / Published: 6 January 2019
(This article belongs to the Special Issue Recent Advances in Nitrogen-Containing Aromatic Heterocycles)
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Abstract

Discovery of novel anticandidal agents with clarified mechanisms of action, could be a rationalist approach against diverse pathogenic fungal strains due to the rise of resistance to existing drugs. In support to this hypothesis, in this paper, a series of benzimidazole-oxadiazole compounds were synthesized and subjected to antifungal activity evaluation. In vitro activity assays indicated that some of the compounds exhibited moderate to potent antifungal activities against tested Candida species when compared positive control amphotericin B and ketoconazole. The most active compounds 4h and 4p were evaluated in terms of inhibitory activity upon ergosterol biosynthesis by an LC-MS-MS method and it was determined that they inhibited ergosterol synthesis concentration dependently. Docking studies examining interactions between most active compounds and lanosterol 14-α-demethylase also supported the in vitro results. View Full-Text
Keywords: benzimidazole; 1,3,4-oxadiazole; antifungal activity; ergosterol biosynthesis; cytotoxicity; molecular docking benzimidazole; 1,3,4-oxadiazole; antifungal activity; ergosterol biosynthesis; cytotoxicity; molecular docking
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Karaburun, A.Ç.; Kaya Çavuşoğlu, B.; Acar Çevik, U.; Osmaniye, D.; Sağlık, B.N.; Levent, S.; Özkay, Y.; Atlı, Ö.; Koparal, A.S.; Kaplancıklı, Z.A. Synthesis and Antifungal Potential of Some Novel Benzimidazole-1,3,4-Oxadiazole Compounds. Molecules 2019, 24, 191.

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