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ID: ALA1132877

Journal: Bioorg Med Chem Lett

Title: Novel alpha-glucosidase inhibitors with a tetrachlorophthalimide skeleton.

Authors: Sou S, Mayumi S, Takahashi H, Yamasaki R, Kadoya S, Sodeoka M, Hashimoto Y.

Abstract: Novel alpha-glucosidase inhibitors with a tetrachlorophthalimide skeleton were prepared and their structure-activity relationships were analyzed. Among them, N-phenyl-4,5,6,7-tetrachlorophthalimide (CPOP: 2) and N-(4-phenylbutyl)-4,5,6,7-tetrachlorophthalimide (CP4P: 6) showed very potent inhibitory activity, being more potent than 1-deoxynojirimycin (dNM: 1). Mechanistic studies revealed that CPOP (2) and CP4P (6) inhibit alpha-glucosidase non-competitively and competitively, respectively.

CiteXplore: 10843222

DOI: 10.1016/s0960-894x(00)00161-x