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

  作者 Goeminne, A; McNaughton, M; Bal, G; Surpateanu, G; Van der Veken, P; De Prol, S; Versees, W; Steyaert, J; Haemers, A; Augustyns, K  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2008年43-2;  页码  315-326  
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[摘要]

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. (c) 2007 Elsevier Masson SAS. All rights reserved.

 
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