Identification of a sulfonamide series of CCR2 antagonists

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 p K a, yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved p...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (13), p.3961-3964
Hauptverfasser:	Peace, Simon, Philp, Joanne, Brooks, Carl, Piercy, Val, Moores, Kitty, Smethurst, Chris, Watson, Steve, Gaines, Simon, Zippoli, Mara, Mookherjee, Claudette, Ife, Robert
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents CCR2 antagonists Dose-Response Relationship, Drug High-Throughput Screening Assays Humans Medical sciences Mice Molecular Structure p Ka Pharmacology. Drug treatments Receptors, CCR1 - antagonists & inhibitors Receptors, CCR2 - antagonists & inhibitors Stereoisomerism Structure-Activity Relationship Sulfonamides Sulfonamides - chemistry Sulfonamides - pharmacology
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Zusammenfassung:	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 p K a, yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.04.142