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.
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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.
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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.
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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.