In vivo activity of an azole series of CCR2 antagonists

Optimisation of a series of biaryl sulphonamides resulted in the identification of compound 7 which demonstrated dose-dependent and strain-specific inhibition of monocyte recruitment in a thioglycollate-induced peritonitis model of inflammation.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-12, Vol.22 (23), p.7252-7255
Hauptverfasser:	Smethurst, Chris A., Bevan, Nicola, Brooks, Carl, Emmons, Amanda, Gough, Peter J., Mookherjee, Claudette, Moores, Kitty, Peace, Simon, Philp, Joanne, Piercy, Val, Watson, Steve P., Zippoli, Mara
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antagonists azoles Azoles - chemical synthesis Azoles - chemistry Azoles - pharmacokinetics Biological and medical sciences CC chemokine receptors CCL2 CCR2 CCR2 protein chemistry Chemokine Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Enzyme System - metabolism Half-Life Inflammation Medical sciences Monocyte chemoattractant protein 1 Monocytes Peritonitis Pharmacology. Drug treatments Protein Binding Rats Receptors, CCR2 - antagonists & inhibitors Receptors, CCR2 - metabolism Structure-Activity Relationship sulfonamides Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - pharmacokinetics Sulphonamides
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Beschreibung
Zusammenfassung:	Optimisation of a series of biaryl sulphonamides resulted in the identification of compound 7 which demonstrated dose-dependent and strain-specific inhibition of monocyte recruitment in a thioglycollate-induced peritonitis model of inflammation.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.09.020