Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines

P C Ting; J F Lee; J C Anthes; N Y Shih; J J Piwinski

doi:10.1016/s0960-894x(00)00464-9

Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2333-5. doi: 10.1016/s0960-894x(00)00464-9.

Authors

P C Ting¹, J F Lee, J C Anthes, N Y Shih, J J Piwinski

Affiliation

¹ Schering-Plough Research Institute, Kenilworth, NJ 07033-1300, USA. [email protected]

PMID: 11055350
DOI: 10.1016/s0960-894x(00)00464-9

Abstract

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.

MeSH terms

Animals
Kinetics
Molecular Structure
Neurokinin-1 Receptor Antagonists*
Piperazines / chemical synthesis*
Piperazines / chemistry
Piperazines / pharmacology
Receptors, Neurokinin-2 / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Neurokinin-1 Receptor Antagonists
Piperazines
Receptors, Neurokinin-2