Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists.
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.
Pharmacopeia Drug Discovery, Inc., PO Box 5350, Princeton, NJ 08543-5350, USA. kanho@pcop.com
Koc-Kan
KK
Ho
Douglas S
DS
Auld
Adolph C
AC
Bohnstedt
Paolo
P
Conti
Wim
W
Dokter
Shawn
S
Erickson
Daming
D
Feng
Jim
J
Inglese
Celia
C
Kingsbury
Steven G
SG
Kultgen
Rong-Qiang
RQ
Liu
Christopher M
CM
Masterson
Michael
M
Ohlmeyer
Yajing
Y
Rong
Martijn
M
Rooseboom
Andrew
A
Roughton
Philippe
P
Samama
Martin-Jan
MJ
Smit
Ellen
E
Son
Jaap
J
van der Louw
Gerard
G
Vogel
Maria
M
Webb
Jac
J
Wijkmans
Ming
M
You
D000284:Administration, Oral; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D008826:Microbial Sensitivity Tests; D011743:Pyrimidines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors
D011743:Pyrimidines; D023063:Receptors, Interleukin-8B; D011994:Recombinant Proteins