Glycosylated dihydrochalcones as potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitors

A series of glucose conjugates was synthesized and tested for inhibition of SGLT1 and SGLT2. The core structure was derived from compound la. Modification of the benzofuran moiety and 4-substituent of the phenyl ring in compound la improved selectivity at SGLT2. Select compounds were compared to la in metabolic stability and in vivo efficacy studies. (C) 2004 Elsevier Ltd. All rights reserved.