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2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 May 15; Vol. 21 (10), pp. 3172-6. Date of Electronic Publication: 2011 Jan 06. - Publication Year :
- 2011
-
Abstract
- TNF-α converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique tridentate fashion. Incorporating (R)-2-(2-N-alkylaminothiazol-4-yl)pyrrolidines into the left hand side amide of the tartrate scaffold led to the discovery of potent and selective TACE inhibitors, some of which exhibited good rat oral bioavailability.<br /> (Copyright © 2011. Published by Elsevier Ltd.)
- Subjects :
- ADAM17 Protein
Amides chemical synthesis
Amides chemistry
Animals
Biological Availability
Enzyme Activation drug effects
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Molecular Structure
Rats
ADAM Proteins antagonists & inhibitors
Amides pharmacology
Enzyme Inhibitors pharmacology
Pyrrolidines chemistry
Tartrates chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21458257
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.01.002