N-Hydroxyformamide peptidomimetics as TACE/Matrix metalloprotease inhibitors: oral activity via P1′ isobutyl substitution

N-Hydroxyformamide peptidomimetics as TACE/Matrix metalloprotease inhibitors: oral activity via P1′ isobutyl substitution

N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and TNF-α converting enzyme (TACE). Compound 13c possesses good oral and intravenous pharmacokinetics in the rat and dog. N-Hydroxyformamide-cla...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-08, Vol.11 (16), p.2147-2151
Hauptverfasser: Musso, David L., Andersen, Marc W., Andrews, Robert C., Austin, Richard, Beaudet, Elizabeth J., Becherer, J.David, Bubacz, Dulce G., Bickett, D.Mark, Chan, Joseph H., Conway, James G., Cowan, David J., Gaul, Michael D., Glennon, Kimberly C., Hedeen, Kevin M., Lambert, Millard H., Leesnitzer, M.Anthony, McDougald, Darryl L., Mitchell, Justin L., Moss, Marcia L., Rabinowitz, Michael H., Rizzolio, Michele C., Schaller, Lee T., Stanford, Jennifer B., Tippin, Timothy K., Warner, Janet R., Whitesell, L.Graham, Wiethe, Robert W.
Format: Artikel
Sprache:eng
Schlagworte:
ADAM Proteins
ADAM17 Protein
Animals
Biological and medical sciences
Dogs
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacokinetics
Enzyme Inhibitors - pharmacology
Formamides - chemistry
Formamides - pharmacology
Matrix Metalloproteinase Inhibitors
Medical sciences
Metalloendopeptidases - antagonists & inhibitors
Miscellaneous
Oligopeptides - chemistry
Oligopeptides - pharmacology
Pharmacology. Drug treatments
Rats
Structure-Activity Relationship
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Zusammenfassung:N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and TNF-α converting enzyme (TACE). Compound 13c possesses good oral and intravenous pharmacokinetics in the rat and dog. N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and TNF-α converting enzyme (TACE). Compound 13c possesses good oral and intravenous pharmacokinetics in the rat and dog.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00377-8