N-Arylmethyl substituted iminoribitol derivatives as inhibitors of a purine specific nucleoside hydrolase

…, G Surpateanu, P Van der Veken, S De Prol…

Index: Goeminne, Annelies; Berg, Maya; McNaughton, Michael; Bal, Gunther; Surpateanu, Georgiana; Van der Veken, Pieter; Prol, Stijn De; Versees, Wim; Steyaert, Jan; Haemers, Achiel; Augustyns, Koen Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6752 - 6763

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Citation Number: 23

Abstract

A key enzyme within the purine salvage pathway of parasites, nucleoside hydrolase, is proposed as a good target for new antiparasitic drugs. We have developed N-arylmethyl- iminoribitol derivatives as a novel class of inhibitors against a purine specific nucleoside hydrolase from Trypanosoma vivax. Several of our inhibitors exhibited low nanomolar activity, with 1, 4-dideoxy-1, 4-imino-N-(8-quinolinyl) methyl-d-ribitol (UAMC-00115, Ki ...