Identification of a sulfonamide series of CCR2 antagonists

Autor:	Simon Peace, Robert J. Ife, Kitty Moores, Claudette Mookherjee, Joanne Philp, Chris A. Smethurst, Carl Brooks, Mara Zippoli, Steve P. Watson, Val Piercy, Simon Gaines
Rok vydání:	2010
Předmět:	Stereochemistry Receptors CCR2 animal diseases Clinical Biochemistry Receptors CCR1 Pharmaceutical Science Stereoisomerism Pharmacology Biochemistry Chemical synthesis Mice Structure-Activity Relationship Pharmacokinetics parasitic diseases Drug Discovery Structure–activity relationship Potency Animals Humans Molecular Biology chemistry.chemical_classification Sulfonamides Dose-Response Relationship Drug Molecular Structure Organic Chemistry Antagonist hemic and immune systems Sulfonamide High-Throughput Screening Assays chemistry Lipophilicity Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 20(13)
ISSN:	1464-3405
Popis:	A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64cae2e02cf27bec7e4593b9f7adde93 https://pubmed.ncbi.nlm.nih.gov/20627722 Zobrazit plný text záznamu Full Text from ScienceDirect