Journal
LETTERS IN DRUG DESIGN & DISCOVERY
Volume 7, Issue 9, Pages 686-693Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157018010792929522
Keywords
Isosteviol; Derivatives; Synthesis; Acute antihyperglycemeric
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Funding
- China Ministry of Health Foundation for Scientific Research [WKJ2005-2-022]
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Isosteviol is a beyerane tetracyclic diterpenoid with a large variety of biological activities. In this article, a series of novel isosteviol derivatives containing the modification of C-18 carboxyl group (5-12), C-16 carbonyl group (14-16) and heteroatom-containing frameworks fused with isosteviol structure (18-19) were synthesized and evaluated for their in vivo acute antihyperglycemeric effects. Among them, compound 8 exhibited the most potent antihyperglycemeric effects. Furthermore, primarily, structure-activity relationship (SAR) was also analyzed. The structures of all the newly synthesized compounds were determined by H-1, (CNMR)-C-13, MS, IR and elementary analysis.
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