Synthesis and α-amylase inhibitory activity of glucose-deoxynojirimycin conjugates
Synthesis and α-amylase inhibitory activity of glucose-deoxynojirimycin conjugates
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DOI：
10.1016/j.tet.2011.08.012
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发表时间：
2011-10-07
期刊：
影响因子：
2.1
通讯作者：
Kawabata, Jun
中科院分区：
文献类型：
--
作者：
Kato, Eisuke;Iwano, Naoya;Kawabata, Jun
α-淀粉酶抑制剂因其假定的抗糖尿病作用而引起人们的关注。尽管许多研究已经探索了天然小分子抑制剂，但阿卡波糖是目前唯一具有足够抑制效力和药物样特征被视为潜在治疗剂的化合物。我们合成了有效的葡萄糖苷酶抑制剂 1-脱氧野尻霉素和葡萄糖的缀合物，旨在增强对 α-淀粉酶的抑制活性。与单独的 1-脱氧野尻霉素相比，这种合成缀合物对 α-淀粉酶的抑制作用增强，表明对现有葡萄糖苷酶抑制剂进行类似修饰可能会产生更有效的 α-淀粉酶抑制剂。 (C) 2011 Elsevier Ltd. 保留所有权利。
Inhibitors of alpha-amylase have attracted attention for their putative effects against diabetes mellitus. Although numerous studies have explored natural small molecule inhibitors, acarbose is currently the only compound with sufficient inhibitory potency and drug-like characteristics to be considered as a potential therapeutic agent. We have synthesized conjugates of the potent glucosidase inhibitor, 1-deoxynojirimycin, and glucose, with the aim of enhancing inhibitory activity against alpha-amylase. This synthetic conjugate showed increased inhibition of alpha-amylase compared to 1-deoxynojirimycin alone, suggesting that similar modifications of existing glucosidase inhibitors may yield more potent alpha-amylase inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.