Development of Thiazolidinones as Fungal Carbonic Anhydrase Inhibitors.

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Date
2020-04-22Author
Carradori, SAngeli, A
Demir-Yazıcı, K
Grande, R
Güzel-Akdemir, Ö
Akdemir, ATİLLA
Supuran, CT
Advisor
Type
Metadata
Show full item recordAbstract
In our efforts to find new and selective thiazolidinone-based anti-Candida agents,
we synthesized and tested 26 thiazolidinones against several Candida spp. and Gram-positive
and Gram-negative bacteria. The compounds showed selective antifungal activity with potency
similar to fluconazole and clotrimazole, while lacking strong antibacterial activity. Molecular docking
and molecular dynamics studies were performed on Candida CYP51a1 and carbonic anhydrase
(CA) enzymes to further suggest putative targets that could mediate the antifungal effects of
these compounds. Finally, the compounds were tested in enzyme inhibition assays to assess their
putative mechanism of action and showed promising KI values in the 0.1–10 µM range against the
Candida glabrata β-CA enzyme CgNce103.
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