Here we synthesized four novel indole conduritol derivatives 1-4 for the first time in the literature and probed their biological activities with the alpha and beta-glucosidases. The compounds showed quite effective glucosidase inhibitory action. IC50 values of the compounds were compared with the known glucosidase inhibitor acarbose and it was determined that newly synthesized indole conduritols had more powerful effect against beta-glucosidase in addition to exhibiting moderate influence against alpha-glucosidase. Our molecules thus constitute an important starting point for the design and exploitation of novel glucosidase inhibitors since glucosidase inhibitors have widespread applications in the treatment of diabetes, viral infections, lysosomal storage diseases and cancers. (C) 2012 Elsevier Ltd. All rights reserved.