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

A Goeminne; M McNaughton; G Bal; G Surpateanu; P Van der Veken; S De Prol; W Versées; J Steyaert; S Apers; A Haemers; K Augustyns

doi:10.1016/j.bmcl.2007.02.017

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

Bioorg Med Chem Lett. 2007 May 1;17(9):2523-6. doi: 10.1016/j.bmcl.2007.02.017. Epub 2007 Feb 9.

Authors

A Goeminne¹, M McNaughton, G Bal, G Surpateanu, P Van der Veken, S De Prol, W Versées, J Steyaert, S Apers, A Haemers, K Augustyns

Affiliation

¹ Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.

PMID: 17317181
DOI: 10.1016/j.bmcl.2007.02.017

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Chemistry, Pharmaceutical / methods*
Drug Design
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Kinetics
Models, Chemical
Molecular Conformation
N-Glycosyl Hydrolases / antagonists & inhibitors*
Ribitol / analogs & derivatives*
Ribitol / chemistry*
Triazoles / chemistry*
Trypanosoma brucei brucei / enzymology

Substances

Enzyme Inhibitors
Triazoles
Ribitol
N-Glycosyl Hydrolases