Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist

Pauline C Ting; Joe F Lee; Neng Yang Shih; John J Piwinski; John C Anthes; Richard W Chapman; Charles A Rizzo; John A Hey; Kwokei Ng; Amin A Nomeir

doi:10.1016/s0960-894x(02)00340-2

Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2125-8. doi: 10.1016/s0960-894x(02)00340-2.

Authors

Pauline C Ting¹, Joe F Lee, Neng Yang Shih, John J Piwinski, John C Anthes, Richard W Chapman, Charles A Rizzo, John A Hey, Kwokei Ng, Amin A Nomeir

Affiliation

¹ The Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. pauline.ting@spcorp.com

PMID: 12127519
DOI: 10.1016/s0960-894x(02)00340-2

Abstract

A novel series of dual NK(1)/NK(2) receptor antagonists, based on the 2-oxo-(1,4'-bipiperidine) template, has been prepared. Compound 10R is a potent dual NK(1)/NK(2) antagonist and demonstrates excellent in vivo activity and good oral plasma levels in the dog.

MeSH terms

Animals
Area Under Curve
Dogs
Drug Evaluation, Preclinical
Guinea Pigs
Molecular Structure
Neurokinin-1 Receptor Antagonists*
Piperidines / blood
Piperidines / chemical synthesis*
Piperidines / chemistry
Piperidines / pharmacology*
Receptors, Neurokinin-2 / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Neurokinin-1 Receptor Antagonists
Piperidines
Receptors, Neurokinin-2