Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.
A series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)- (methoxyimino)pentyl-1-piperazines was prepared and their affinity for the NK1 and NK2 receptors investigated. Compounds 7f, 10o, 10r, and 10s were found to be our most potent inhibitors.
Ting
P C
PC
Schering-Plough Research Institute, Kenilworth, NJ 07033-1300, USA. pauline.ting@spcorp.com
Lee
J F
JF
Anthes
J C
JC
Shih
N Y
NY
Piwinski
J J
JJ
D000818:Animals; D007700:Kinetics; D015394:Molecular Structure; D064729:Neurokinin-1 Receptor Antagonists; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D064729:Neurokinin-1 Receptor Antagonists; D010879:Piperazines; D018041:Receptors, Neurokinin-2