Concise syntheses of selective inhibitors against α-1,3-galactosyltransferase.
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.
Zhang
Guo-Liang
GL
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, and School of Pharmaceutical Sciences, Peking University, Xue Yuan Road #38, Beijing 100191, China.
Zhang
Li-He
LH
Ye
Xin-Shan
XS
D002236:Carbohydrate Conformation; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D005700:Galactosyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D013379:Substrate Specificity / Q000187:drug effects; D014531:Uridine Diphosphate Galactose / Q000737:chemistry / Q000378:metabolism
D004791:Enzyme Inhibitors; D014531:Uridine Diphosphate Galactose; D005700:Galactosyltransferases