首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Evaluation of the inhibitory potential of five squaric acid derivatives against pancreatic lipase
【24h】

Evaluation of the inhibitory potential of five squaric acid derivatives against pancreatic lipase

机译:评价五种方酸衍生物对胰腺脂肪酶的抑制潜力

获取原文
           

摘要

A series of 4-alkylamino-2-ethoxycyclobut-3en-1,2-diones has been synthesized, characterized and their inhibitory effect on pancreatic lipase (PL) was evaluated. The compound 1 has shown relatively high potency (IC50?=?0.11?mM) compared with the most effective anti-obesity drug, tetrahydrolipstatin (Orlistat) (IC50 value?=?0.08?mM). The compounds have showed good selectivity toward PL and did not affect the activity of trypsin, another digestive enzyme.
机译:合成了一系列的4-烷基氨基-2-乙氧基环丁-3en-1,2-二酮,表征了其对胰腺脂肪酶(PL)的抑制作用。与最有效的抗肥胖药四氢lipstatin(Orlistat)(IC 50 值)相比,化合物1具有相对较高的效价(IC 50 ?=?0.11?mM) ?=?0.08?mM)。这些化合物对PL表现出良好的选择性,并且不影响另一种消化酶胰蛋白酶的活性。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号