Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371077 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
The asymmetric synthesis of 1-C-alkyl-l-arabinoiminofuranoses 1 was achieved by asymmetric allylic alkylation (AAA), ring closing metathesis (RCM), and Negishi cross coupling as key reactions. Some of the prepared compounds showed potent inhibitory activities towards intestinal maltase, with IC50 values comparable to those of commercial drugs such as acarbose, voglibose, and miglitol, which are used in the treatment of type 2 diabetes. Among them, the inhibitory activity (IC50 = 0.032 μM) towards intestinal sucrase of 1c was quite strong compared to the above commercial drugs.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yoshihiro Natori, Tatsushi Imahori, Keiichi Murakami, Yuichi Yoshimura, Shinpei Nakagawa, Atsushi Kato, Isao Adachi, Hiroki Takahata,