期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 7, 页码 1762-1765出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.02.032
关键词
Anti-diabetic activity; Type 2 diabetes mellitus; 12-(Substituted aminomethyl) berberrubine derivatives; Synthesis
资金
- National Science Foundation of China [81373259]
- Science & Technology Pillar Program of Sichuan Province of China [2011SZ0014]
By introducing various amino methyl groups into 12-position of berberrubine, a series of 12-(substituted aminomethyl) berberrubine derivatives were synthesized and evaluated for their anti-diabetic activity against type 2 diabetes mellitus. The results indicated that most of the prepared compounds exhibited moderate to good anti-diabetic activity, which were comparable to or even better than the berberine, the positive control rosiglitazone and insulin. Especially, compound 3b with an N-methyl piperazine-4-methyl group at C-12, exerted the most powerful anti-diabetic activity. (C) 2014 Elsevier Ltd. All rights reserved.
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