Synthesis And Preliminary Evaluation Of Antidiabetic Activity Of 4-(1-Aryl-3-Aryl/Arylalkyl-3-Oxopropylamino)-N-(5-Methyl-3-Isoxazolyl)Be Nzene Sulfonamide
CHINESE JOURNAL OF ORGANIC CHEMISTRY(2009)
Abstract
To explore novel peroxisome proliferator-activated receptor (PPAR) agonists with high efficacy and low toxicity, thirteen new beta-amino ketone derivatives containing a sulfamethoxazole moiety were synthesized directly through Mannich reaction in the yields of 39.8%similar to 92.5%. Their structures were characterized by IR, H-1 NMR, C-13 NMR, ESI MS and HRMS techniques. The preliminary bioassay showed that compound la could activate PPAR response element obviously. The reaction conditions and the structure-activity relationship of these compounds were also discussed.
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Key words
PPAR,Mannich reaction,beta-amino ketone derivative,sulfamethoxazole,diabetes mellitus
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