Synthesis of all stereoisomers of 3-hydroxypipecolic acid and 3-hydroxy-4,5-dehydropipecolic acid and their evaluation as glycosidase inhibitors.
作者信息
Ohara Chiaki, Takahashi Ryouko, Miyagawa Tatsunori, Yoshimura Yuichi, Kato Atsushi, Adachi Isao, Takahata Hiroki
机构信息
Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, Sendai 981-8558, Japan.
出版信息
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1810-3. doi: 10.1016/j.bmcl.2008.02.028. Epub 2008 Feb 14.
PMID:18296050
Abstract
A highly practicable synthesis of both enantiomers of 3-hydroxypipecolic acid derivatives 1, 2, 3, 4 is described. Screening of these molecules for glycosidase inhibition has been examined. Compound 3 was shown to be a potent inhibitor of beta-N-acetylglucosaminidase as well as Escherichia coli beta-glucuronidase.
摘要
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