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Bioorg Med Chem Lett. 2004 Feb 23;14(4):1043-8.

Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.

Author information

1
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Quebec H9R 4P8, Canada. lau@merck.com

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.

PMID:
15013020
DOI:
10.1016/j.bmcl.2003.11.076
[Indexed for MEDLINE]

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