Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 6, Pages 2015-2022Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.01.052
Keywords
Neoponkoranol; Neosalaprinol; alpha-Glucosidase inhibitor; Salacia; SAR study
Funding
- MEXT (Ministry of Education, Culture, Sports, Science and Technology)
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Two hitherto missing members of sulfonium salts family in Salacia genus plants as a new class of a-glucosidase inhibitors, neoponkoranol (7) and neosalaprinol (8), were isolated from the water extracts, and their structures were unambiguously identified. For further SAR studies on this series of sulfonium salts, several epimers of 7 and 8 were synthesized, and their inhibitory activities against rat small intestinal alpha-glucosidases were evaluated. Among them, 3'-epimer of 7 was found most potent in this class of molecules, and revealed as potent as currently used antidiabetics, voglibose and acarbose. (C) 2011 Elsevier Ltd. All rights reserved.
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