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Anticandidal properties of N-acylpeptides containing an inhibitor of glucosamine-6-phosphate synthase |
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| Authors: | Ryszard Andruszkiewicz Teresa Zieniawa Aleksandra Walkowiak |
| Institution: | 1. Department of Pharmaceutical Technology and Biochemistry, Gdańsk University of Technology, 11/12 Narutowicza Street, 80-952, Gdańsk, Polandryszarda@chem.pg.gda.pl;3. Department of Pharmaceutical Technology and Biochemistry, Gdańsk University of Technology, 11/12 Narutowicza Street, 80-952, Gdańsk, Poland |
| Abstract: | A series of N-acyl peptides 1–9, containing an inhibitor of glucosamine-6-phosphate synthase have been synthesised and tested against Candida strains. N-Acylated peptides inhibit glucosamine-6-phosphate synthase in cell free extracts from Candida albicans. Antifungal activities of the tested compounds correlated with their lipophilic properties. Peptides acylated with decanoic acid were found to be the most potent in the series. N-decanoylpeptides also showed activity against Candida albicans Gu5 resistant mutant with Cdr1 and Cdr2 drug extrusion proteins that causes MDR by an active efflux mechanism. |
| Keywords: | Antifungal activity glucosamine-6-phosphate synthase inhibition N-acyl peptides |