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Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Dec 15; Vol. 20 (24), pp. 7283-7. Date of Electronic Publication: 2010 Oct 23. - Publication Year :
- 2010
-
Abstract
- Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors with good DMPK profiles.<br /> (Published by Elsevier Ltd.)
- Subjects :
- ADAM Proteins metabolism
ADAM17 Protein
Acetylene analogs & derivatives
Acetylene pharmacokinetics
Acetylene therapeutic use
Animals
Anti-Inflammatory Agents pharmacokinetics
Anti-Inflammatory Agents therapeutic use
Dogs
Haplorhini
Humans
Protease Inhibitors pharmacokinetics
Protease Inhibitors therapeutic use
Rats
ADAM Proteins antagonists & inhibitors
Anti-Inflammatory Agents chemistry
Arthritis, Rheumatoid drug therapy
Protease Inhibitors chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21106451
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.10.081