Design, synthesis and biological evaluation of hetaryl-nucleoside derivatives as inhibitors of chitin synthase

JB Behr, T Gourlain, A Helimi, G Guillerm

Index: Behr, Jean-Bernard; Gourlain, Thierry; Helimi, Abdellatif; Guillerm, Georges Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 10 p. 1713 - 1716

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Citation Number: 59

Abstract

We report here the design, synthesis and biological evaluation of new models of sugar analogues for chitin synthase. These UDP-GlcNAc mimetics associate a sugar-mimicking hetaryl group and uridine, linked with different pyrophosphate bioisosteres. The compounds displayed weak inhibition activity on chitin synthase and their antifungal potencies have been assayed against a large variety of pathogenic fungi.