Synthesis and biological evaluation of gem-diamine 1-N-iminosugars related to L-iduronic acid as inhibitors of heparan sulfate 2-O-sulfotransferase.

Synthesis and biological evaluation of gem-diamine 1-N-iminosugars related to L-iduronic acid as inhibitors of heparan sulfate 2-O-sulfotransferase.
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与L-艾杜糖醛酸相关的偕二胺1-N-亚氨基糖作为硫酸乙酰肝素2-O-磺基转移酶抑制剂的合成和生物学评价。

DOI:
10.1016/j.bmcl.2005.10.055
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发表时间:
2006
期刊:
Bioorganic & medicinal chemistry letters.
影响因子:
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通讯作者:
Esko,JeffreyD
Esko,JeffreyD
中科院分区:
--
文献类型:
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作者:
Brown,JillianR;Nishimura,Yoshio;Esko,JeffreyD

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合成了一系列与L-艾杜糖醛酸相关的宝石二胺1-N-亚氨基葡萄糖,并用体外酶试验评价了它们对硫酸乙酰肝素糖醛酸基2-O-磺酸转移酶的抑制作用。两个含有胍基的亚氨糖在体外是该酶的有效抑制剂。
A variety of gem-diamine 1-N-iminosugars related to l-iduronic acid were synthesized and evaluated as inhibitors of heparan sulfate uronyl 2-O-sulfotransferase using an in vitro enzyme assay. Two iminosugars containing guanidino groups acted as potent in vitro inhibitors of the enzyme.