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Mono, di and tri-mannopyranosyl phosphates as mannose-1-phosphate prodrugs for potential CDG-Ia therapy.

作者信息

Hardré Renaud, Khaled Amira, Willemetz Alexandra, Dupré Thierry, Moore Stuart, Gravier-Pelletier Christine, Le Merrer Yves

机构信息

Université René Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints-Pères, 75006 Paris, France.

出版信息

Bioorg Med Chem Lett. 2007 Jan 1;17(1):152-5. doi: 10.1016/j.bmcl.2006.09.074. Epub 2006 Oct 17.

DOI:10.1016/j.bmcl.2006.09.074
PMID:17049852
Abstract

An efficient and convergent method for the synthesis of mannose-1-phosphate prodrugs is described as a potential therapy for congenital disorders of glycosylation-Ia (CDG-Ia). The key feature of the proposed approach is the silver assisted nucleophilic substitution of 2,3,4,6-tetra-O-protected-alpha-d-mannopyranosyl bromides with various silver phosphate salts to afford mono, di, and tri-mannopyranosyl phosphates. A preliminary biological evaluation of the synthesized phosphate prodrugs has been carried out.

摘要

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