Title | Synthesis and biochemical evaluation of guanidino-alkyl-ribitol derivatives as nucleoside hydrolase inhibitors. |
Publication Type | Journal Article |
Year of Publication | 2008 |
Authors | Goeminne, A., M. McNaughton, G. Bal, G. Surpateanu, P. Van der Veken, S. De Prol, W. Versées, J. Steyaert, A. Haemers, and K. Augustyns |
Journal | Eur J Med Chem |
Volume | 43 |
Issue | 2 |
Pagination | 315-26 |
Date Published | 2008 Feb |
ISSN | 0223-5234 |
Keywords | Animals, Drug Evaluation, Preclinical, Enzyme Inhibitors, Magnetic Resonance Spectroscopy, Models, Molecular, N-Glycosyl Hydrolases, Spectrometry, Mass, Electrospray Ionization, Trypanosoma vivax |
Abstract | Nucleoside hydrolase (NH) is a key enzyme in the purine salvage pathway. The purine specificity of the IAG-NH from Trypanosoma vivax is at least in part due to cation-pi-stacking interactions. Guanidinium ions can be involved in cation-pi-stacking interactions, therefore a series of guanidino-alkyl-ribitol derivatives were synthesized in order to examine the binding affinity of these compounds towards the target enzyme. The compounds show moderate to good inhibiting activity towards the IAG-NH from T. vivax. |
DOI | 10.1016/j.ejmech.2007.03.027 |
Alternate Journal | Eur J Med Chem |
PubMed ID | 17582660 |
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