Synthesis of novel β-amino ketones containing a p-aminobenzoic acid moiety and evaluation of their antidiabetic activities |
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作者姓名: | TANG GuangXia YAN JuFang FAN Li XU Jin SONG XiaoLi JIANG Li LUO LingFei YANG DaCheng |
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作者单位: | School of Chemistry and Chemical Engineering, Southwest University;Drug Screening Center, Chengdu Di Ao Pharmaceutical Group Co., Ltd.;Schlumberger Technology Corporation;School of Life Science, Southwest University |
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基金项目: | the Natural Science Foundation of Chongqing (2005BB5095);the Ph.D Research Foundation of Southwest University (SWNU, B2005010);the Scientific and Technological Project in Chongqing (CSTC, 2011AB5001) for financial support |
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摘 要: | The synthesis of two series of β-amino ketones containing a p-aminobenzoic acid moiety (TM-1 and TM-2) using a modified protocol of the Mannich reaction is reported. The molecular structures of a total of tweenty three new target compounds were characterized by 1H NMR, 13C NMR, ESI-MS and HR-MS. Subsequently, their antidiabetic activities were screened in vitro. The α-glucodase inhibition (α-GI) activity of compound 1e reached a remarkable level of 66.50%. The peroxisome proliferatoractivated receptor (PPAR) relative activation activities of six compounds are above 80%, and in particular 2i displays an unprecedentedly high PPAR of 130.91%. The structure-activity relationships of the compounds were established. 2i is also subject to further in-depth investigation.
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关 键 词: | diabetes mellitus α-glucosidase peroxisome proliferator-activated receptor β-amino ketone Mannich reaction |
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