Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok, Thailand.
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1538-40. doi: 10.1016/j.bmcl.2012.01.007. Epub 2012 Jan 10.
An effective synthesis of (+)-conduritol F, (+)-chiro- and (+)-epi-inositols from naturally available (+)-proto-quercitol is described. This synthetic method provides a concise synthesis of cyclitols in enantiomerically pure form. Of the synthesized cyclitols, (+)-conduritol F potently inhibits type I α-glucosidase with an IC(50) value of 86.1 μM, which is five times greater than the standard antidiabetic drug, acarbose.
从天然存在的 (+)-表儿茶醇出发，有效合成了 (+)-古洛糖醇 F、(+)-手性和 (+)-表-肌醇。该合成方法为环糖醇的对映体纯形式的简洁合成提供了可能。在所合成的环糖醇中，(+)-古洛糖醇 F 对 I 型 α-葡萄糖苷酶具有很强的抑制作用，IC50 值为 86.1 μM，是标准抗糖尿病药物阿卡波糖的五倍。
