Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors
Cheuk K Lau1, Christopher I Bayly, Jacques Yves Gauthier
1Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Quebec H9R 4P8, Canada. lau@merck.com
Bioorganic & Medicinal Chemistry Letters
|March 12, 2004
Abstract:
A series of benzotriazole phenyldifluoromethylphosphonic acids were found to be potent PTP-1B inhibitors. Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphatase.

