1.
Bioorg Med Chem Lett
; 20(12): 3557-60, 2010 Jun 15.
Article
in English
| MEDLINE
| ID: mdl-20529684
ABSTRACT
A series of phenyl piperidine 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, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.
Subject(s)
Matrix Metalloproteinase Inhibitors , Administration, Oral , Animals , Biological Availability , Hydroxamic Acids/administration & dosage , Matrix Metalloproteinase 1/drug effects , Matrix Metalloproteinase 14/drug effects , Piperidines , Rats , Small Molecule Libraries , Solubility , Substrate Specificity , Sulfones
2.
Bioorg Med Chem Lett
; 20(12): 3561-4, 2010 Jun 15.
Article
in English
| MEDLINE
| ID: mdl-20529685
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.