Synthesis of phenylalkyl-substituted polyhydroxypiperidines as potent inhibitors for α-l-fucosidase
作者:Tomoki Saka、Toru Okaki、Shohei Ifuku、Yukiko Yamashita、Kasumi Sato、Shota Miyawaki、Akiko Kamori、Atsushi Kato、Isao Adachi、Yasuhiro Tezuka、Peter G. Kiria、Osamu Onomura、Daishiro Minato、Kenji Sugimoto、Yuji Matsuya、Naoki Toyooka
DOI:10.1016/j.tet.2013.10.006
日期:2013.12
Synthesis and inhibitory activities against alpha-L-fucosidase of phenylalkyl-substituted polyhydroxy piperidines have been described. Among the newly synthesized compounds, 2,4,6-trichloro derivative (16q) showed very high inhibitory activity against alpha-L-fucosidase with IC50 value of 0.005 mu M, and K-i values of 0.0011 mu M, respectively. (C) 2013 Elsevier Ltd. All rights reserved.