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Articles 1 - 4 of 4
Full-Text Articles in Physical Sciences and Mathematics
Alpha-Alkyl-Alpha-Amino-Beta-Sulphone Hydroxamates As Potent Mmp Inhibitors That Spare Mmp-1, Daniel Becker, Gary A. Decrescenzo, John Freskos, Daniel P. Getman
Alpha-Alkyl-Alpha-Amino-Beta-Sulphone Hydroxamates As Potent Mmp Inhibitors That Spare Mmp-1, Daniel Becker, Gary A. Decrescenzo, John Freskos, Daniel P. Getman
Daniel P. Becker
A series of α-alkyl-α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-2 and MMP-13, and for selectivity versus MMP-1. Low nanomolar potency was obtained with selectivity versus MMP-1 ranging from >10 to >1000. Selected compounds were orally bioavailable.
Orally Bioavailable Dual Mmp-1/Mmp-14 Sparing, Mmp-13 Selective Alpha-Sulfone Hydroxamates, Daniel Becker, Stephen A. Kolodziej, Susan L. Hockerman, Terri L. Boehm, Jeffery N. Carroll
Orally Bioavailable Dual Mmp-1/Mmp-14 Sparing, Mmp-13 Selective Alpha-Sulfone Hydroxamates, Daniel Becker, Stephen A. Kolodziej, Susan L. Hockerman, Terri L. Boehm, Jeffery N. Carroll
Daniel P. Becker
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, Stephen A. Kolodziej, Susan L. Hockerman, Gary A. Decrescenzo, Joseph J. Mcdonald, Grace E. Munie, Theresa R. Fletcher, Nathan Stehle, Craig Swearingen, Daniel Becker
Mmp-13 Selective Isonipecotamide Alpha-Sulfone Hydroxamates, Stephen A. Kolodziej, Susan L. Hockerman, Gary A. Decrescenzo, Joseph J. Mcdonald, Grace E. Munie, Theresa R. Fletcher, Nathan Stehle, Craig Swearingen, Daniel Becker
Daniel P. Becker
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.
Mmp-13 Selective Alpha-Sulfone Hydroxamates: Identification Of Selective P1' Amides, Yvette M. Fobian, John N. Freskos, Thomas E. Barta, Louis J. Bedell, Daniel Becker
Mmp-13 Selective Alpha-Sulfone Hydroxamates: Identification Of Selective P1' Amides, Yvette M. Fobian, John N. Freskos, Thomas E. Barta, Louis J. Bedell, Daniel Becker
Daniel P. Becker
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we report on a series of hydroxamic acids with a flexible amide P1' substituents. We identify an amide which spares both MMP-1 and -14, and shows >500 fold selectivity for MMP-13 versus MMP-2 and -8.