Discovery of potent, selective and orally bioavailable triaryl-sulfonamide based PTP1B inhibitors

A novel series of DFMP/DFMS/ISD containing triaryl-sulfonamide derivatives (5a-r) are reported as potent PTP1B inhibitors. Some of the test compounds exhibits good selectivity towards PTP1B over various PTPs, including TCPTP (in vitro) and the lead compound 5o shows excellent antidiabetic activity (in vivo).