Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

Autor:	Christine A. Collins, Mei Liu, Hongyu Zhao, Rich S. Janis, Heidi S. Camp, Teresa K. Surowy, Gang Liu, Bo Liu, Nelson Lissa T, Harriet T. Smith, Ning Cao, Tom S. Suhar, Michael D. Serby, Zhili Xin, Hing L. Sham, Bruce G. Szczepankiewicz
Rok vydání:	2008
Předmět:	Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Substrate Specificity Structure-Activity Relationship chemistry.chemical_compound Piperidines In vivo Drug Discovery medicine Urea Structure–activity relationship Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Aryl Organic Chemistry Stearoyl-CoA Desaturase Enzyme chemistry Molecular Medicine lipids (amino acids peptides and proteins) Piperidine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:4298-4302
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.06.088
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::055af8cecf34aa640b107ce18838c33e https://doi.org/10.1016/j.bmcl.2008.06.088 Zobrazit plný text záznamu Full Text from ScienceDirect