Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase

Autor:	Martin A. Lewis, Louis S. Chupak, Robert G. Gentles, Shuanghua Hu, Min Ding, Yazhong Huang, Xiaofan Zheng, Yuval Blat, Andrea McClure, Ryan Westphal
Rok vydání:	2015
Předmět:	0301 basic medicine Diacylglycerol lipase Stereochemistry Clinical Biochemistry 2-Arachidonoylglycerol Glycine Pharmaceutical Science Biochemistry 03 medical and health sciences chemistry.chemical_compound Structure-Activity Relationship 0302 clinical medicine Drug Discovery Structure–activity relationship Humans Enzyme Inhibitors Molecular Biology Diacylglycerol kinase chemistry.chemical_classification Lipoprotein lipase Sulfonamides biology Dose-Response Relationship Drug Molecular Structure Organic Chemistry Lipoprotein Lipase 030104 developmental biology Enzyme chemistry Covalent bond Lipase inhibitors biology.protein Molecular Medicine lipids (amino acids peptides and proteins) 030217 neurology & neurosurgery
Zdroj:	Bioorganicmedicinal chemistry. 24(7)
ISSN:	1464-3391
Popis:	N-Benzylic-substituted glycine sulfonamides that reversibly inhibit diacylglycerol (DAG) lipases are reported. Detailed herein are the structure activity relationships, profiling characteristics and physico-chemical properties for the first reported series of DAG lipase (DAGL) inhibitors that function without covalent attachment to the enzyme. Highly potent examples are presented that represent valuable tool compounds for studying DAGL inhibition and constitute important leads for future medicinal chemistry efforts.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e63ae0d200553eec7d772a4bac3e9f9 https://pubmed.ncbi.nlm.nih.gov/26917221 Zobrazit plný text záznamu Full Text from ScienceDirect