Bioorganic & medicinal chemistry, 2008-08, Vol.18 (15), p.4298-4302
2008
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Details
- Autor(en) / Beteiligte
- Titel
- Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry, 2008-08, Vol.18 (15), p.4298-4302
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2008
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- The discovery of potent, selective, orally bioavailable SCD1 inhibitors is reported. A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure–activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors. 4-(2-Chlorophenoxy)- N-[3-(methyl carbamoyl)phenyl]piperidine-1-carboxamide 4c exhibited robust in vivo activity with dose-dependent desaturation index lowering effects.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894X, 0968-0896eISSN: 1464-3405, 1464-3391DOI: 10.1016/j.bmcl.2008.06.088Titel-ID: cdi_proquest_miscellaneous_69359626
- Format
- –
- Schlagworte
- Biological and medical sciences, Desaturation index, Dose-Response Relationship, Drug, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, General and cellular metabolism. Vitamins, Medical sciences, Molecular Structure, Pharmacology. Drug treatments, Piperidines - chemical synthesis, Piperidines - chemistry, Piperidines - pharmacology, SCD1 inhibitors, Stearoyl-CoA Desaturase - antagonists & inhibitors, Structure-Activity Relationship, Substrate Specificity, Urea - analogs & derivatives, Urea - chemical synthesis, Urea - chemistry, Urea - pharmacology