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首页> 外文期刊>Heterocycles: An International Journal for Reviews and Communications in Heterocyclic Chemistry >SYNTHESES AND EVALUATION AS GLYCOSIDASE INHIBITOR OF 1,5-DIDEOXY-1,5-IMINO-D-GLUCITOL ANALOGS OF SALACINOL, A POTENT α-GLUCOSIDASE INHIBITOR ISOLATED FROM AYURVEDIC MEDICINE, SALACIA RETICULATA
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SYNTHESES AND EVALUATION AS GLYCOSIDASE INHIBITOR OF 1,5-DIDEOXY-1,5-IMINO-D-GLUCITOL ANALOGS OF SALACINOL, A POTENT α-GLUCOSIDASE INHIBITOR ISOLATED FROM AYURVEDIC MEDICINE, SALACIA RETICULATA

机译:AL草素的1,5-二恶英-1,5-亚氨基-D-葡糖醇类似物的糖苷酶抑制剂的合成及评价

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摘要

N-Alkylated deoxynojirimycin (10) bearing the same alkyl chain as salacinol (1), a potent oc-glucosidase inhibitor isolated from Ayurvedic traditional medicine, Salacia reticulata, was found to inhibit both rat intestinal maltase and sucrase as strong as 1, while 10 has been reported to be inactive against glucoamylase G2 from Aspergillus niger. Its O-desulfate (12) was also found active against these enzymes, and characteristic sulfate anion moiety of 1 was found not essential for the oc-glucosidase inhibitory activity.
机译:N-烷基化的脱氧野oji霉素(10)与Salacinol(1)具有相同的烷基链,这是一种从阿育吠陀传统药物Salacia reticulata中分离出来的有效的oc-葡萄糖苷酶抑制剂,可抑制大鼠肠内的麦芽糖酶和蔗糖酶,其抑制力高达1,而10据报道对黑曲霉的葡糖淀粉酶G2无活性。还发现其O-脱硫酸盐(12)对这些酶有活性,并且发现特征性硫酸根阴离子部分1对oc-葡萄糖苷酶抑制活性不是必需的。

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