Amidine derived inhibitors of acid-sensing ion channel-3 (ASIC3).
A series of indole amidines modified at the 2-position of the indole ring were evaluated as inhibitors of Acid-Sensing Ion Channel-3 (ASIC3), a novel target for the treatment of chronic pain.
Kuduk
Scott D
SD
Department of Medicinal Chemistry, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. scott_d_kuduk@merck.com
Chang
Ronald K
RK
Wai
Jenny M-C
JM
Di Marco
Christina N
CN
Cofre
Victoria
V
DiPardo
Robert M
RM
Cook
Sean P
SP
Cato
Matthew J
MJ
Jovanovska
Aneta
A
Urban
Mark O
MO
Leitl
Michael
M
Spencer
Robert H
RH
Kane
Stefanie A
SA
Hartman
George D
GD
Bilodeau
Mark T
MT
D062565:Acid Sensing Ion Channels; D000578:Amidines / Q000737:chemistry*; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004594:Electrophysiology; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D007473:Ion Channels / Q000737:chemistry; D008297:Male; D008956:Models, Chemical; D009288:Naproxen / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D015222:Sodium Channels / Q000737:chemistry*; D013329:Structure-Activity Relationship
C112231:ASIC3 protein, human; D062565:Acid Sensing Ion Channels; D000578:Amidines; D007211:Indoles; D007473:Ion Channels; D015222:Sodium Channels; D009288:Naproxen