Concise syntheses of selective inhibitors against α-1,3-galactosyltransferase
Guo-Liang Zhang1, Li-He Zhang1, Xin-Shan Ye1
1State Key Laboratory of Natural and Biomimetic Drugs, Peking University, and School of Pharmaceutical Sciences, Peking University, Xue Yuan Road #38, Beijing 100191, China. xinshan@bjmu.edu.cn.
Abstract:
Several iminosugar-based uridine diphosphate galactose (UDP-Gal) mimetics 1-4 including d- and l-epimers were designed and synthesized by concise routes, and these synthetic compounds were evaluated for the inhibition of α-1,3- and β-1,4-galactosyltransferases in vitro. The experimental data demonstrated that l-epimer 2 displayed the strongest inhibitory activity with moderate selectivity against α-1,3-galactosyltransferase.
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