Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (7), p.2370-2374
2010
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: Part 1
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (7), p.2370-2374
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A series of pyrazole-based thioethers were prepared and found to be potent cathepsin S inhibitors. A crystal structure of 13 suggests that the thioether moiety may bind to the S3 pocket of the enzyme. Additional optimization led to the discovery of aminoethylthioethers with improved enzymatic activity and submicromolar cellular potency.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.01.108Titel-ID: cdi_proquest_miscellaneous_745930625
- Format
- –
- Schlagworte
- Binding Sites, Biological and medical sciences, Cathepsin, Cathepsins - antagonists & inhibitors, Cathepsins - chemistry, Cathepsins - metabolism, Cell Line, Crystallography, X-Ray, Humans, Immunomodulators, Medical sciences, Models, Molecular, Pharmacology. Drug treatments, Protease, Protease Inhibitors - chemistry, Protease Inhibitors - pharmacology, Pyrazoles - chemistry, Pyrazoles - pharmacology, Structure-Activity Relationship, Sulfides - chemistry, Sulfides - pharmacology, Thioether