Bioorganic & medicinal chemistry letters, 2003-10, Vol.13 (19), p.3243-3246
2003
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and biological activity of piperazine-Based dual MMP-13 and TNF-α converting enzyme inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2003-10, Vol.13 (19), p.3243-3246
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2003
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A series of novel MMP-13 and TNF-α converting enzyme inhibitors based on piperazine 2-hydroxamic acid scaffolds are described. The TACE, MMP-1 and MMP-13 activity of these inhibitors as well as the effect of substitution of the piperazine nitrogen and the P-1′ benzyloxy tailpiece is discussed. Moderate in vivo activity is observed with several members of this group. A series of novel piperazine-based hydroxamic acids with potent TACE activity is described.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/S0960-894X(03)00666-8Titel-ID: cdi_proquest_miscellaneous_73605307
- Format
- –
- Schlagworte
- ADAM Proteins, ADAM17 Protein, Animals, Biological and medical sciences, Bones, joints and connective tissue. Antiinflammatory agents, Collagenases - metabolism, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - pharmacology, Matrix Metalloproteinase 13, Matrix Metalloproteinase Inhibitors, Medical sciences, Metalloendopeptidases - antagonists & inhibitors, Metalloendopeptidases - metabolism, Pharmacology. Drug treatments, Piperazines - chemical synthesis, Piperazines - pharmacology, Rats, Tumor Necrosis Factor-alpha - metabolism