Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5222995 | Tetrahedron | 2009 | 8 Pages |
Abstract
Botryllazine B analogues of diverse substitution patterns have been prepared, and their in vitro inhibitory activities against recombinant human aldose reductase (h-ALR2) evaluated. Among the 15 compounds tested, 6-(4-aminophenyl)-2-(4-hydroxyphenyl)carbonylpyrazine (7b) proved to be the most potent inhibitor, with IC50=0.91 μM. Kinetic analyses of 7b and botryllazine B (1) revealed that these inhibitors exhibit an unprecedented mixed-type inhibition on h-ALR2 with respect to the substrate d,l-glyceraldehyde, in the presence of NADPH at inhibitor concentrations near the IC50 values.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ryota Saito, Mai Tokita, Keisuke Uda, Chikako Ishikawa, Mitsutoshi Satoh,