Add to ORKGSeeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Letter on a series of hydroxamic acids with a flexible benzamide tail groups.(1a) Here, we replace the amide moiety with non-hydrolyzable heterocycles in an effort to improve half-life. We identify a hydroxamate tetrazole 4e that spares MMP-1 and -14, shows \u3e400-fold selectivity versus MMP-8 and \u3e600-fold selectivity versus MMP-2, and has a 4.8 h half-life in rats. X-ray data (1.9 Å) for tetrazole 4c is presented
Matrix metalloproteinase-13 (MMP-13) is a key enzyme implicated in the degradation of the extracellu...
A series of novel, MMP-1 sparing arylhydroxamate sulfonamides with activity against MMP-2 and -13 is...
To evaluate N-hydroxyurea as zinc binding group in the design of MMP inhibitors, two peptidyl 1-hydr...
Seeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Lette...
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we re...
A series of N-aryl isonipecotamide α-sulfone hydroxamate derivatives has been prepared utilizing a c...
A series of α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and...
A series of α-alkyl-α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MM...
A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combin...
The matrix metalloproteinase enzyme MMP-13 plays a key role in the degradation of type II collagen i...
This letter describes SAR exploration and rat PK optimization of a series of novel, MMP-1 sparing ar...
Matrix metalloproteinases (MMPs) are a family of zinc dependent endopeptidases known to play key rol...
A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated as matri...
α-Piperidine-β-sulfone hydroxamate derivatives were explored that are potent for matrix metalloprote...
As the matrix metalloproteinases (MMPs) can be massively up-regulated in degenerative tissues and de...
Matrix metalloproteinase-13 (MMP-13) is a key enzyme implicated in the degradation of the extracellu...
A series of novel, MMP-1 sparing arylhydroxamate sulfonamides with activity against MMP-2 and -13 is...
To evaluate N-hydroxyurea as zinc binding group in the design of MMP inhibitors, two peptidyl 1-hydr...
Seeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Lette...
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we re...
A series of N-aryl isonipecotamide α-sulfone hydroxamate derivatives has been prepared utilizing a c...
A series of α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and...
A series of α-alkyl-α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MM...
A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combin...
The matrix metalloproteinase enzyme MMP-13 plays a key role in the degradation of type II collagen i...
This letter describes SAR exploration and rat PK optimization of a series of novel, MMP-1 sparing ar...
Matrix metalloproteinases (MMPs) are a family of zinc dependent endopeptidases known to play key rol...
A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated as matri...
α-Piperidine-β-sulfone hydroxamate derivatives were explored that are potent for matrix metalloprote...
As the matrix metalloproteinases (MMPs) can be massively up-regulated in degenerative tissues and de...
Matrix metalloproteinase-13 (MMP-13) is a key enzyme implicated in the degradation of the extracellu...
A series of novel, MMP-1 sparing arylhydroxamate sulfonamides with activity against MMP-2 and -13 is...
To evaluate N-hydroxyurea as zinc binding group in the design of MMP inhibitors, two peptidyl 1-hydr...