Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (7), p.2375-2378
2010
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Details
- Autor(en) / Beteiligte
- Titel
- Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (7), p.2375-2378
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A novel class of tetrahydropyrido-pyrazole thioether amines that display potency against human Cathepsin S have been previously reported. Here, further SAR investigations of the P3, P4, and P5 regions are described. In particular, 4-fluoropiperidine is identified as a competent P3 binding element when utilized in conjunction with a ( S)-2-hydroxypropyl linker-containing P5 moiety and oxamide or sulfonamide P4 substitution.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.01.104Titel-ID: cdi_proquest_miscellaneous_745931374
- Format
- –
- Schlagworte
- Biological and medical sciences, Cathepsin S, Cathepsins - antagonists & inhibitors, Cathepsins - metabolism, Cell Line, Humans, Immunomodulators, Inhibitor, Medical sciences, Pharmacology. Drug treatments, Protease Inhibitors - chemistry, Protease Inhibitors - pharmacology, Pyrazole, Pyrazoles - chemistry, Pyrazoles - pharmacology, Structure-Activity Relationship, Sulfides - chemistry, Sulfides - pharmacology