Synthesis and biochemical evaluation of guanidino-alkyl-ribitol derivatives as nucleoside hydrolase inhibitors.

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.

journal_name

Eur J Med Chem

authors

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

doi

10.1016/j.ejmech.2007.03.027

subject

Has Abstract

pub_date

2008-02-01 00:00:00

pages

315-26

issue

2

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00160-2

journal_volume

43

pub_type

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