Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 7, Pages 2252-2262Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.02.028
Keywords
Kotalanol; alpha-Glucosidase inhibitor; Salacia; SAR study; Selective inhibition
Funding
- High-Tech Research Center, MEXT (Ministry of Education, Culture, Sports, Science and Technology)
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Synthesis and evaluation of four diastereomers (9a, 9b, 9c and 9d) of kotalanol, a potent alpha-glucosidase inhibitor isolated from an Ayurvedic medicinal plant Salacia species, are described. Stereo-inversion at C-3' and C-4' of kotalanol (2) caused significant decrease of the inhibitory activities against maltase and sucrase, whereas inhibitory activity against isomaltase sustained, thus resulted in exerting selectivity against isomaltase. (C) 2011 Elsevier Ltd. All rights reserved.
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