MMP-13 selective isonipecotamide alpha-sulfone hydroxamates

Stephen A Kolodziej; Susan L Hockerman; Gary A DeCrescenzo; Joseph J McDonald; Debbie A Mischke; Grace E Munie; Theresa R Fletcher; Nathan Stehle; Craig Swearingen; Daniel P Becker

doi:10.1016/j.bmcl.2010.04.111

MMP-13 selective isonipecotamide alpha-sulfone hydroxamates

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3561-4. doi: 10.1016/j.bmcl.2010.04.111. Epub 2010 Apr 28.

Authors

Stephen A Kolodziej¹, Susan L Hockerman, Gary A DeCrescenzo, Joseph J McDonald, Debbie A Mischke, Grace E Munie, Theresa R Fletcher, Nathan Stehle, Craig Swearingen, Daniel P Becker

Affiliation

¹ Department of Medicinal Chemistry, Pfizer Research & Development, St. Louis, MO 63198, USA.

PMID: 20529685
DOI: 10.1016/j.bmcl.2010.04.111

Abstract

A series of N-aryl isonipecotamide alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13.

MeSH terms

Administration, Oral
Amides
Animals
Hydroxamic Acids / chemical synthesis
Hydroxamic Acids / chemistry*
Hydroxamic Acids / pharmacology
Inhibitory Concentration 50
Matrix Metalloproteinase Inhibitors*
Rats
Small Molecule Libraries
Solubility
Substrate Specificity
Sulfones

Substances

Amides
Hydroxamic Acids
Matrix Metalloproteinase Inhibitors
Small Molecule Libraries
Sulfones