Abstract
The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue degradation. These enzymes are strictly regulated by endogenous inhibitors such as tissue inhibitors of MMPs and α2-macroglobulins. Overexpression of these enzymes has been implicated in various pathological disorders such as arthritis, tumor metastasis, cardiovascular diseases, and multiple sclerosis. Developing effective small-molecule inhibitors to modulate MMP activity is one approach to treat these degenerative diseases. The present work focuses on the discovery and SAR of novel N-hydroxy-α-phenylsulfonylacetamide derivatives, which are potent, selective, and orally active MMP inhibitors.
Original language | English |
---|---|
Pages (from-to) | 2361-2375 |
Number of pages | 15 |
Journal | Journal of Medicinal Chemistry |
Volume | 46 |
Issue number | 12 |
DOIs | |
State | Published - Jun 5 2003 |
Externally published | Yes |