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