Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome

Autor:	Simon D.P. Baugh, Praveen K. Pabba, Joseph Barbosa, Eric Coulter, Urvi Desai, Jason P. Gay, Suma Gopinathan, Qiang Han, Rajee Hari, S. David Kimball, Huy V. Nguyen, Chi-You Ni, David R. Powell, Arian Smith, Kristen M. Terranova, Alan Wilson, Xuan-Chuan Yu, Victoria K. Lombardo
Rok vydání:	2015
Předmět:	Fatty Acid Desaturases Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry Mice Structure-Activity Relationship chemistry.chemical_compound Delta-5 Fatty Acid Desaturase In vivo Drug Discovery medicine Animals Humans Enzyme Inhibitors Molecular Biology Delta 5 desaturase Metabolic Syndrome chemistry.chemical_classification Indazole Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry medicine.disease Amides In vitro Enzyme Liver Design synthesis Drug Design Molecular Medicine Metabolic syndrome
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 25:3836-3839
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2015.07.066
Popis:	The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole series displayed in vivo activity in reducing the enzymatic activity of liver delta-5 desaturase.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34d3a2e8a2feeee1565ab9c579d48d8f https://doi.org/10.1016/j.bmcl.2015.07.066 Zobrazit plný text záznamu Full Text from ScienceDirect