Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Cinnamides as novel CCR1 antagonist chemotypes are described with high affinity to human and rodent receptors. A1B1 and A4B7 showed oral activity in the mouse collagen induced arthritis.
Revesz
Laszlo
L
Novartis Institutes for BioMedical Research, Global Discovery Chemistry, Autoimmunity and Transplantation, CH-4002 Basel, Switzerland. Laszlo.revesz@novartis.com
Bollbuck
Birgit
B
Buhl
Thomas
T
Eder
Joerg
J
Esser
Ronald
R
Feifel
Roland
R
Heng
Richard
R
Hiestand
Peter
P
Jachez-Demange
Benedicte
B
Loetscher
Pius
P
Sparrer
Helmut
H
Schlapbach
Achim
A
Waelchli
Rudolf
R
D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry* / Q000627:therapeutic use*; D001169:Arthritis, Experimental / Q000188:drug therapy*; D006801:Humans; D051379:Mice; D051381:Rats; D054389:Receptors, CCR1; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; C515300:CCR1 protein, human; C515301:Ccr1 protein, mouse; C515302:Ccr1 protein, rat; D054389:Receptors, CCR1; D019707:Receptors, Chemokine