| Literature DB >> 22189136 |
Dipam Patel1, Mukul Jain, Shailesh R Shah, Rajesh Bahekar, Pradip Jadav, Amit Joharapurkar, Nirav Dhanesha, Mubeen Shaikh, Kalapatapu V V M Sairam, Prashant Kapadnis.
Abstract
A novel series of pTyr mimetics containing triaryl-sulfonamide derivatives (5a-r) are reported as potent and selective PTP1B inhibitors. Some of the test compounds (5o and 5p) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro). The lead compound 5o showed potent antidiabetic activity (in vivo), along with improved pharmacokinetic profile. These preliminary results confirm discovery of highly potent and selective PTP1B inhibitors for the treatment of T2DM.Entities:
Mesh：
Substances：
Year: 2011 PMID： 22189136 DOI： 10.1016/j.bmcl.2011.11.122
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823