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

Publication Type:

Journal Article

Authors:

Goeminne,A.; McNaughton,M.; Bal,G.; Surpateanu,G.; Van,Der,V; De,Prol S.; Versees,W.; Steyaert,J.; Haemers,A.; Augustyns,K.

Source:

Eur. Journ. Med. Chem., Volume 43, Issue 2, p.315 - 326 (2008)

URL:

PM:17582660

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

Notes:

DA - 20080215
IS - 0223-5234 (Print)
LA - eng
PT - Journal Article
SB - IM