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Development of Thiazolidinones as Fungal Carbonic Anhydrase Inhibitors.

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132-10.3390-ijms21082960.pdf (4.157Mb)
Date
2020-04-22
Author
Carradori, S
Angeli, A
Demir-Yazıcı, K
Grande, R
Güzel-Akdemir, Ö
Akdemir, ATİLLA
Supuran, CT
Advisor
Type
Article
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Abstract
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.
Subject
Güzel-Akdemir Ö., Carradori S., Grande R., Demir-Yazıcı K., Angeli A., Supuran C., Akdemir A., -Development of Thiazolidinones as Fungal Carbonic Anhydrase Inhibitors.-, International journal of molecular sciences, cilt.21, 2020
URI
https://hdl.handle.net/20.500.12645/17996
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BEZMIALEM VAKIF UNIVERSITY

About us |Policies | Library | Contact us | Send Feedback | Sitemap | Admin

Bezmialem Vakıf Üniversitesi, Adnan Menderes Bulvarı Vatan Caddesi 34093 Fatih, İstanbul / TURKEY
Copyright © Bezmialem Vakıf Üniversitesi

Creative Commons Lisansı
Bezmialem Institutional Repository, Creative Commons Alıntı-GayriTicari-Türetilemez 4.0 Uluslararası Lisansı ile lisanslanmıştır.

OpenAccess@BVU

Support by  UNIREPOS