Sulfonamido-aryl ethers as bradykinin B1 receptor antagonists.
The synthesis and identification of sulfonamido-aryl ethers as potent bradykinin B1 receptor antagonists from a approximately 60,000 member encoded combinatorial library are reported. Two distinct series of compounds exhibiting different structure-activity relationships were identified in a bradykinin B1 whole-cell receptor-binding assay. Specific examples exhibit K(i) values of approximately 10nM.
Cole
Andrew G
AG
Pharmacopeia Inc, Princeton, NJ 08543, USA. acole@pcop.com
Metzger
Axel
A
Brescia
Marc-Raleigh
MR
Qin
Lan-Ying
LY
Appell
Kenneth C
KC
Brain
Christopher T
CT
Hallett
Allan
A
Ganju
Pam
P
Denholm
Alastair A
AA
Wareing
James R
JR
Ritchie
Timothy J
TJ
Drake
Gillian M
GM
Bevan
Stuart J
SJ
MacGloinn
Aisling
A
McBryde
Andrew
A
Patel
Viral
V
Oakley
Paul J
PJ
Nunez
Ximena
X
Gstach
Hubert
H
Schneider
Peter
P
Baldwin
John J
JJ
Dolle
Roland E
RE
McDonald
Edward
E
Henderson
Ian
I
D000818:Animals; D065169:Bradykinin B1 Receptor Antagonists; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques; D004987:Ethers / Q000138:chemical synthesis*; D006801:Humans; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
D065169:Bradykinin B1 Receptor Antagonists; D004987:Ethers; D054852:Small Molecule Libraries; D013449:Sulfonamides