1,2,3-Triazolylalkylribitol derivatives as nucleoside hydrolase inhibitors.

Title1,2,3-Triazolylalkylribitol derivatives as nucleoside hydrolase inhibitors.
Publication TypeJournal Article
Year of Publication2007
AuthorsGoeminne, A., M. McNaughton, G. Bal, G. Surpateanu, P. Van der Veken, S. De Prol, W. Versées, J. Steyaert, S. Apers, A. Haemers, and K. Augustyns
JournalBioorg Med Chem Lett
Volume17
Issue9
Pagination2523-6
Date Published2007 May 1
ISSN0960-894X
KeywordsAnimals, Chemistry, Pharmaceutical, Drug Design, Enzyme Inhibitors, Kinetics, Models, Chemical, Molecular Conformation, N-Glycosyl Hydrolases, Ribitol, Triazoles, Trypanosoma brucei brucei
Abstract

A range of novel 1,2,3-triazolylalkylribitol derivatives were synthesized and evaluated as nucleoside hydrolase inhibitors. The most active compound (11a) has low micromolar potency and is structurally diverse from previously reported nucleoside hydrolase inhibitors, which, along with the simplicity of the chemistry involved in its synthesis, makes it a good lead for the further development of novel nucleoside hydrolase inhibitors.

DOI10.1016/j.bmcl.2007.02.017
Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID17317181