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Note | Regular issue | Vol 48, No. 11, 1998, pp.2365-2378
Published online, 1st January, 1970
DOI: 10.3987/COM-98-8289
Synthesis and Activity as a Glycosidase Inhibitor of 2,8-Dihydroxyindolizidines

Ho Seong Na, Jaehyuck Choi, Jaehoon Yu, Kye Jung Shin, Kyung Ho Yoo, Dong Jin Kim,* and Sang Woo Park*

*Medicinal Chemistry Research Center, Korea Institute of Science and Technology, P.O. Box 131, Cheongryang, Seoul 130-650, Korea


The synthesis and enzyme assay of 2,8-dihydroxyindolizidines (5) were described. Four diastereomers of these were prepared from trans-4-hydroxy-L-proline (6) which is commercially available amino acid. Among synthetic compounds 5a1 and 5b2 showed medium potent inhibition to α-amyloglycosidase, while 5a2 displayed medium activity to α-glucosidase.