Synthesis of novel β-amino ketones containing a p-aminobenzoic acid moiety and evaluation of their a

• 作 者: TANG GuangXia YAN JuFang FAN Li XU Jin SONG XiaoLi JIANG Li LUO LingFei YANG DaCheng
• 机 构: School of Chemistry and Chemical Engineering, Southwest University,Drug Screening Center, Chengdu Di
• 出 处: Science China(Chemistry)
• 发表日期: 2013年04期
• 关键词: moiety aldehydes aromatic substituent PPAR screened chloroform substituted steri

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.

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 The peroxisome was characterized by 1H NMR, 13C NMR, ESI-MS and HR-MS. The anti-diabetic activity was screened in vitro. The α-glucodase inhibition (α-GI) activity of compound 1e reached a remarkable level of 66.50%. The structure-activity relationships of the compounds were established. 2i is also subject to further in-depth investigation (PPAR) relative activation activities of six compounds are above 80%, and in particular 2i displays an unprecedentedly high PPAR of 130.91%. .