N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution

Autor:	Marcia L. Moss, David J. Cowan, Bubacz Dulce Garrido, Timothy K. Tippin, Stanford Jennifer Badiang, Michele C. Rizzolio, Robert W. Wiethe, Darryl Lynn Mcdougald, Lee T. Schaller, Joseph H. Chan, James G. Conway, Millard H. Lambert, Justin L. Mitchell, Robert Carl Andrews, M. Anthony Leesnitzer, David Lee Musso, Janet Warner, Andersen Marc W, Michael H. Rabinowitz, J. David Becherer, Kimberly C. Glennon, D. Mark Bickett, Michael D. Gaul, L.Graham Whitesell, Elizabeth J. Beaudet, Richard Austin, Kevin M. Hedeen
Rok vydání:	2001
Předmět:	Peptidomimetic Stereochemistry Clinical Biochemistry Pharmaceutical Science Matrix metalloproteinase ADAM17 Protein Matrix Metalloproteinase Inhibitors Biochemistry Structure-Activity Relationship Dogs Pharmacokinetics Oral administration Drug Discovery Animals Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Metalloproteinase biology Formamides Chemistry Organic Chemistry Metalloendopeptidases In vitro Rats ADAM Proteins Enzyme Enzyme inhibitor biology.protein Molecular Medicine Oligopeptides
Zdroj:	Bioorganicmedicinal chemistry letters. 11(16)
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e45088b93c91fa2f5b7cc63b35d439d5 https://pubmed.ncbi.nlm.nih.gov/11514157 Zobrazit plný text záznamu Full Text from ScienceDirect