文章基本信息

标题：Synthesis and Aldose Reductase Inhibitory Activity of Botryllazine A Derivatives
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作者：Ryota Saito ; Kana Ishibashi ; Maiko Noumi 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2019
卷号：67
期号：6
页码：556-565
DOI：10.1248/cpb.c19-00003
出版社：The Pharmaceutical Society of Japan
摘要：Aldose reductase (AR) is associated with the onset of diabetic complications. Botryllazine A and its analogues were synthesized and evaluated for human AR inhibitory activity. Analogues possessing aromatic bicyclic systems at the C5 position of the central pyrazine ring exhibited superior AR inhibiting activity relative to the parent botryllazine A. In addition, the benzoyl groups at positions C2 and C3 of the pyrazine ring were dispensable for this improved inhibitory activity. Conversely, a benzoyl group—containing phenolic hydroxyl groups—at either position C2 or C3 of the pyrazine ring was essential for attainment of high inhibitory activity approaching that of sorbinil (a highly effective AR inhibitor).
关键词：aldose reductase (AR);aldose reductase inhibitor (ARI);diabetic complication;botryllazine A;pyrazine;docking study