New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase.

New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase.

Bioorg Chem. 2015 May 22;61:13-20

Authors: Kral K, Bieg T, Nawrot U, Włodarczyk K, Lalik A, Hahn P, Wandzik I

Abstract
This study described the synthesis and in vitro evaluation of eight new derivatives of uridine as antifungal agents and inhibitors of chitin synthase. Dimeric uridinyl derivatives synthesized by us did not exhibit significant activity. One of the studied monomeric derivative, 5'-(N-succinyl)-5'-amino-5'-deoxyuridine methyl ester (compound 7) showed activities against several fungal strains (MIC range 0.06-1.00mg/mL) and inhibited chitin synthase from Saccharomyces cerevisiae (IC50=0.8mM). Moreover compound 7 exhibited synergistic interaction with caspofungin against Candida albicans (FIC index=0.28).

PMID: 26051755 [PubMed - as supplied by publisher]