New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists

…, AWJ Cooper, R Bell, IJM Beresford…

Index: Smith, Paul W.; Cooper, Anthony W. J.; Bell, Richard; Beresford, Isabel J. M.; Gore, Paul M.; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 19 p. 3772 - 3779

Full Text: HTML

Citation Number: 36

Abstract

The synthesis of a series of 2-(5-fluoro-W-indol-3-yl) ethyl spiropiperidines is described together with their tachykinin NK2 receptor affinities measured in a rat colon binding assay. Equivalent NK2 receptor binding affinity was observed for the spirooxazolidinone 3-benzyl-8- [2-(5-fluoro-~-indol-3-yl) ethyll-l-oxa-3, 8-diazaspiro [4.5 ldecan-2-one (Sa), the imidazolidinone 3-benzyl-8-[2-(5-fluoro-~-indol-3-yl) ethyll-l, 3, 8-triazaspiro~ 4.5 ldecan-2 ...