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Synthesis of phenylalkyl-substituted polyhydroxypiperidines as potent inhibitors for α-l-fucosidase

Authors :
Shota Miyawaki
Kenji Sugimoto
Toru Okaki
Yasuhiro Tezuka
Atsushi Kato
Daishiro Minato
Yuji Matsuya
Kasumi Sato
Osamu Onomura
Akiko Kamori
Shohei Ifuku
Tomoki Saka
Peter G. Kiria
Isao Adachi
Naoki Toyooka
Yukiko Yamashita
Source :
Tetrahedron. 69:10653-10661
Publication Year :
2013
Publisher :
Elsevier BV, 2013.

Abstract

Synthesis and inhibitory activities against α- l -fucosidase of phenylalkyl-substituted polyhydroxypiperidines have been described. Among the newly synthesized compounds, 2,4,6-trichloro derivative (16q) showed very high inhibitory activity against α- l -fucosidase with IC50 value of 0.005 μM, and Ki values of 0.0011 μM, respectively.

Details

ISSN :
00404020
Volume :
69
Database :
OpenAIRE
Journal :
Tetrahedron
Accession number :
edsair.doi...........beb11fcb328cf4daafb39897642ce556
Full Text :
https://doi.org/10.1016/j.tet.2013.10.006