4.3 Article

Synthesis of New α-Glucosidase Inhibitors Based on Oleanolic Acid Incorporating Cinnamic Amides

期刊

CHEMICAL & PHARMACEUTICAL BULLETIN
卷 59, 期 8, 页码 1051-1056

出版社

PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.59.1051

关键词

synthesis; alpha-glucosidase inhibitor; oleanolic acid; cinnamic amide

资金

  1. National Natural Science Foundation of China for Outstanding Young Scientists [30525032]
  2. National Natural Science Foundation of China [81073009]
  3. National Key Scientific and Technological Special Projects [2009ZX09502-011]

向作者/读者索取更多资源

A series of a-glucosidase inhibitors with the oleanolic acid core and different cinnamic amide ligands were designed and synthesized. Their preliminary structure activity relationships were analyzed. In general, the compounds with 3,28-disubstituted oleanolic acid exhibited stronger activity than those 28-monosubstituted analogues, and variation of cinnamic amide substitution significantly affected alpha-glucosidase inhibition activities. Most of the compounds showed potent inhibitory activity against alpha-glucosidase with much greater efficacy than a typical alpha-glucosidase inhibitor, acarbose.

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