期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 24, 页码 6877-6881出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.088
关键词
O-Spiroketal C-arylglucosides; SGLT2; Spiro[isobenzofuran-1, 2 '-pyran]; Glucosuria; Blood glucose
A series of novel O-spiroketal C-arylglucosides have been prepared and evaluated in cell-based functional assays for activity against human sodium-dependent glucose co-transporters 1 and 2 ( SGLT1 and 2). The core spiro[isobenzofuran-1,2'-pyran] structure proved to be an effective scaffold for diversification and a number of compounds with single digit nanomolar potency and high selectivity have been synthesized. Compound 5a promoted glucosuria when administered in vivo in rats and produced a significant blood glucose reduction effect. (C) 2009 Elsevier Ltd. All rights reserved.
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