Goeminne A, McNaughton M, Bal G, Surpateanu G, Van der Veken P, De Prol S, Versées W, Steyaert J, Apers S, Haemers A, Augustyns K
Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
Bioorg Med Chem Lett. 2007 May 1;17(9):2523-6. doi: 10.1016/j.bmcl.2007.02.017. Epub 2007 Feb 9.
A range of novel 1,2,3-triazolylalkylribitol derivatives were synthesized and evaluated as nucleoside hydrolase inhibitors. The most active compound (11a) has low micromolar potency and is structurally diverse from previously reported nucleoside hydrolase inhibitors, which, along with the simplicity of the chemistry involved in its synthesis, makes it a good lead for the further development of novel nucleoside hydrolase inhibitors.
合成了一系列新型的1,2,3 - 三唑基烷基核糖醇衍生物，并将其作为核苷水解酶抑制剂进行了评估。活性最高的化合物（11a）具有低微摩尔活性，且在结构上与先前报道的核苷水解酶抑制剂不同，再加上其合成过程中涉及的化学反应简单，这使其成为新型核苷水解酶抑制剂进一步开发的良好先导化合物。
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