In vivo activity of an azole series of CCR2 antagonists.
Optimisation of a series of biaryl sulphonamides resulted in the identification of compound 14 [corrected] which demonstrated dose-dependent and strain-specific inhibition of monocyte recruitment in a thioglycollate-induced peritonitis model of inflammation. [Formula: see text]. [corrected].
GlaxoSmithKline Research and Development, Medicines Research Centre, Stevenage, UK.
Chris A
CA
Smethurst
Nicola
N
Bevan
Carl
C
Brooks
Amanda
A
Emmons
Peter J
PJ
Gough
Claudette
C
Mookherjee
Kitty
K
Moores
Simon
S
Peace
Joanne
J
Philp
Val
V
Piercy
Steve P
SP
Watson
Mara
M
Zippoli
D000284:Administration, Oral; D000818:Animals; D001393:Azoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D006207:Half-Life; D011485:Protein Binding; D051381:Rats; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
D001393:Azoles; D065607:Cytochrome P-450 Enzyme Inhibitors; D054390:Receptors, CCR2; D013449:Sulfonamides; D003577:Cytochrome P-450 Enzyme System