The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2

Autor:	Colin A. Leach, Colin H. Macphee, V.Ann Lewis, Kevin J. Milliner, Ivan Leo Pinto, Ian Stansfield, Robert J. Ife, Caroline M. Whittaker, Beverley Hammond, Helen F. Boyd, Deirdre Mary Bernadette Hickey, Stephen A. Smith, Colin J. Theobald
Rok vydání:	2001
Předmět:	Male medicine.drug_class Arteriosclerosis Clinical Biochemistry Pharmaceutical Science Carboxamide Pyrimidinones Biochemistry Phospholipases A chemistry.chemical_compound Phospholipase A2 Drug Discovery medicine Potency Animals Humans Pyrimidone Enzyme Inhibitors Molecular Biology chemistry.chemical_classification biology Molecular Structure Chemistry Lipoprotein-associated phospholipase A2 Drug Administration Routes Organic Chemistry Water In vitro Rats Phospholipases A2 Enzyme Solubility Enzyme inhibitor biology.protein Molecular Medicine Rabbits
Zdroj:	Bioorganicmedicinal chemistry letters. 11(5)
ISSN:	0960-894X
Popis:	Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phospholipase A2, has given inhibitors of nanomolar potency and improved physicochemical properties. Compound 23 was identified as a potent, highly water soluble, CNS penetrant inhibitor suitable for intravenous administration.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33b9f3a4a8b9227e0e3cf823d002f5ae https://pubmed.ncbi.nlm.nih.gov/11266173 Zobrazit plný text záznamu Full Text from ScienceDirect