N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.
It has been hypothesized that peripherally restricted NMDA receptor antagonists may be effective analgesics for osteoarthritis pain. A class of novel quinoxalinedione atropisomers, first discovered for an NMDA receptor antagonist program for the treatment of stroke, was evaluated and further optimized with the goal of finding peripherally restricted NMDA receptor antagonists.
Deur
Christopher
C
Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. christopher.deur@pfizer.com
Agrawal
Arun K
AK
Baum
Heidi
H
Booth
John
J
Bove
Susan
S
Brieland
Joan
J
Bunker
Amy
A
Connolly
Cleo
C
Cornicelli
Joseph
J
Dumin
JoAnn
J
Finzel
Barry
B
Gan
Xinmin
X
Guppy
Sheila
S
Kamilar
Gregg
G
Kilgore
Kenneth
K
Lee
Pil
P
Loi
Cho-Ming
CM
Lou
Zhen
Z
Morris
Mark
M
Philippe
Laurence
L
Przybranowski
Sally
S
Riley
Frank
F
Samas
Brian
B
Sanchez
Brian
B
Tecle
Haile
H
Wang
Ziqiang
Z
Welch
Kathryn
K
Wilson
Michael
M
Yates
Karen
K
D000700:Analgesics / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D019540:Area Under Curve; D001665:Binding Sites; D008958:Models, Molecular; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy; D011485:Protein Binding; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000097:blood / Q000737:chemistry* / Q000494:pharmacology*
D000700:Analgesics; D016194:Receptors, N-Methyl-D-Aspartate; D013449:Sulfonamides