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  • Title: Stereoselective synthesis of bioactive isosteviol derivatives as alpha-glucosidase inhibitors.
    Author: Wu Y, Yang JH, Dai GF, Liu CJ, Tian GQ, Ma WY, Tao JC.
    Journal: Bioorg Med Chem; 2009 Feb 15; 17(4):1464-73. PubMed ID: 19167896.
    Abstract:
    Considerable interest has been attracted in isosteviol and its derivatives because of their large variety of pharmacological activities. In this project, a series of novel compounds containing hydroxyl, hydroxymethyl group and heteroatom-containing frameworks fused with isosteviol structure were synthesized and evaluated as alpha-glucosidase inhibitors, aimed at clarifying the structure-activity correlation. The results indicated that these isosteviol derivatives were capable of inhibiting in vitro alpha-glucosidase with moderate to good activities. Among them, indole derivative 15b exhibited the highest activities and thus may be exploitable as a lead compound for the development of potent alpha-glucosidase inhibitors.
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