Sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors are the current focus on the indication for the management of hyperglycemia in diabetes. Here, a novel series of C- linked indolylxyloside-based inhibitors of SGLT2 has been discovered. Structure–activity relationship studies revealed that substituents at the 7-position of the indole moiety and a p- cyclopropylphenyl group in the distal position were necessary for optimum inhibitory ...