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Abstract
A molecular umbrella composed of two O‐sulfated cholic acid residues was applied for the construction of conjugates with cispentacin, containing a “trimethyl lock” (TML) or o‐dithiobenzylcarbamoyl moiety as a cleavable linker. Three out of five conjugates demonstrated antifungal in vitro activity against C. albicans and C. glabrata but not against C. krusei, with MIC90 values in the 0.22–0.99 mM range and were not hemolytic. Antifungal activity of the most active conjugate 24c, containing the TML–pimelate linker, was comparable to that of intact cispentacin. A structural analogue of 24c, containing the Nap‐NH2 fluorescent probe, was accumulated in Candida cells, and TML‐containing conjugates were cleaved in cell‐free extract of C. albicans cells. These results suggest that a molecular umbrella can be successfully applied as a nanocarrier for the construction of cleavable antifungal conjugates.
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- Publication version
- Accepted or Published Version
- DOI:
- Digital Object Identifier (open in new tab) 10.3390/molecules26185475
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- Category:
- Articles
- Type:
- artykuły w czasopismach
- Published in:
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MOLECULES
no. 26,
ISSN: 1420-3049 - Language:
- English
- Publication year:
- 2021
- Bibliographic description:
- Skwarecki A., Martynow D., Milewska M., Milewski S.: Molecular Umbrella as A Nanocarrier for Antifungals// MOLECULES -Vol. 26,iss. 18 (2021), s.5475-
- DOI:
- Digital Object Identifier (open in new tab) 10.3390/molecules26185475
- Verified by:
- Gdańsk University of Technology
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