Synthesis of NAM-thiazoline derivatives as novel O-GlcNAcase inhibitors.

Hanchu Kong,Wei Chen,Tian Liu,Huizhe Lu,Qing Yang,Yanhong Dong,Xiaomei Liang,Shuhui Jin,Jianjun Zhang

Carbohydrate Research（2016）

引用 12|浏览15

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摘要

•Ten novel NAM-thiazoline derivatives have been synthesized for the first time as a new type of inhibition for human O-GlcNAcase.•Several compounds have shown good inhibitory activity for human O-GlcNAcase (IC50 < 15 μM).•One inhibitor exhibited more than 150-fold selectivity for hOGA over hHex.

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关键词

β-N-Acetyl-D-hexosaminidases,NAM-thiazoline derivatives,O-GlcNAcase,Selective inhibitors

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