4-(1-芳基-3-烃基-3-氧代丙胺基)-N-(5-甲基-3-异噁唑基)苯磺酰胺的合成与抗糖尿病活性的初步研究  

Synthesis and Preliminary Evaluation of Antidiabetic Activity of 4-(1-Aryl-3-aryl/arylalkyl-3-oxopropylamino)-N-(5-methyl-3-isoxazolyl)benzene Sulfonamide

作　　者：宋小礼[1] 晏菊芳 范莉[1] 陈欣 许荩[1] 周祖文[1] 杨大成[1] 

机构地区：[1]西南大学化学化工学院,重庆400715 [2]成都地奥制药集团药物筛选中心,成都610041

出　　处：《有机化学》2009年第4期606-613,共8页Chinese Journal of Organic Chemistry

基　　金：重庆市自然科学基金(No.CSTC2005BB5095);西南师范大学博士科研基金(No.SWNU.B2005010);高新技术培育基金(No.XSGX05)资助项目.

摘　　要：为寻找新型高效低毒的过氧化物酶体增殖物激活受体(PPAR)激动剂,通过Mannich反应一步合成了13个含有磺胺甲噁唑结构单元的未见报道的β-氨基酮衍生物,收率为39.8%～92.5%.化合物的结构通过IR,1HNMR,13CNMR,ESIMS和HRMS表征.生物活性测试结果表明,化合物1a能够显著激活PPAR反应元件.文中还对合成反应条件及化合物结构-活性关系进行了初步讨论.To explore novel peroxisome proliferator-activated receptor （PPAR） agonists with high efficacy and low toxicity, thirteen new β-amino ketone derivatives containing a sulfamethoxazole moiety were synthesized directly through Mannich reaction in the yields of 39.8%-92.5%. Their structures were characterized by IR, ^1H NMR, ^13C 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.

关 键 词：过氧化物酶体增殖物激活受体 MANNICH反应 β-氨基酮衍生物 磺胺甲噁唑 糖尿病 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]