5 research outputs found
Orally Bioavailable Dual MMP-1/MMP-14 Sparing, MMP-13 Selective Alpha-sulfone Hydroxamates
A series of phenyl piperidine α-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
MMP-13 Selective Isonipecotamide Alpha-sulfone Hydroxamates
A series of N-aryl isonipecotamide α-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
α-Amino-β-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1
A series of α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and selectivity versus MMP-1. Various substituents were employed on the α-amino group (P1 position), as well as different groups attached to the sulphone group extending into P1′. Low nanomolar potency was obtained for MMP-13 with selectivity versus MMP-1 of \u3e1000× for a number of analogues.
α-Amino-β-sulphone hydroxamates were prepared, which are potent MMP-13 inhibitors with selectivity versus MMP-1 of \u3e1000× for a number of analogues. Selected compounds exhibited oral bioavailability