Synthesis and Anticandidal Activities of Some Aryl (5-Chloro-Benzofuran- 2-yl) Ketoximes

Author(s): Ahmet Cagri Karaburun*

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 4 , 2019

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Graphical Abstract:


Background: In this study, some aryl (5-chloro-benzofuran-2-yl) ketoximes and their ethers were synthesised to evaluate their antifungal activity against C. albicans, C. glabrata, C. krusei, and C. parapsilosis.

Methods: The structure elucidation of the compounds was performed by IR, 1H-NMR, 13C-NMR and HR-MS spectroscopic data. ADME parameters of synthesised compounds 2a-2d, 3a-3d, 4a-4d were predicted by an in-silico study and it was determined that all synthesised compounds may have a good pharmacokinetic profile.

Results: In the anticandidal activity studies, compounds 2c and 3c were found to be the most active compounds. The effect of compound 2c, on ergosterol biosynthesis of C. albicans, was determined by using the LC-MS-MS method.

Conclusion: It was also docked in the active site of the lanosterol 14α-demethylase enzyme, and shown that there is a strong interaction between compound 2c and enzyme.

Keywords: Aryl (5-chloro-benzofuran-2-yl) ketoximes, Anticandidal activity, Ergosterol inhibition, 14-alpha demethylase, docking study, antifungal activity.

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Year: 2019
Page: [427 - 436]
Pages: 10
DOI: 10.2174/1570180816666181207155701
Price: $65

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