Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors

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

doi:10.1016/s0960-894x(00)00702-2

Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors

Bioorg Med Chem Lett. 2001 Feb 26;11(4):491-4. doi: 10.1016/s0960-894x(00)00702-2.

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. pauline.ting@spcorp.com

PMID: 11229755
DOI: 10.1016/s0960-894x(00)00702-2

Abstract

The NK1 and NK2 receptor activity of a series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)-(methoxyimino)pentyl-1-piperidines was evaluated. Compounds 11d, 11e, 11f, 12a, and 12k were found to be our most potent inhibitors.

MeSH terms

Neurokinin-1 Receptor Antagonists*
Piperidines / chemical synthesis*
Piperidines / pharmacology
Receptors, Neurokinin-2 / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Neurokinin-1 Receptor Antagonists
Piperidines
Receptors, Neurokinin-2