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

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 simplicit...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (9), p.2523-2526
Hauptverfasser:	Goeminne, A., McNaughton, M., Bal, G., Surpateanu, G., Van der Veken, P., De Prol, S., Versées, W., Steyaert, J., Apers, S., Haemers, A., Augustyns, K.
Format:	Artikel
Sprache:	eng
Schlagworte:	1,2,3-Triazolylalkylribitol 1,3-Dipolar cycloaddition Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Biological and medical sciences Chemistry, Pharmaceutical - methods Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Kinetics Medical sciences Models, Chemical Molecular Conformation N-Glycosyl Hydrolases - antagonists & inhibitors Nucleoside hydrolase inhibitors Pharmacology. Drug treatments Ribitol - analogs & derivatives Ribitol - chemistry Triazoles - chemistry Trypanosoma brucei brucei - enzymology
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.02.017