1,2,3-TRISUBSTITUTED CYCLOHEXYL SUBSTANCE-P ANTAGONISTS - SIGNIFICANCE OF THE RING NITROGEN IN PIPERIDINE-BASED NK-1 RECEPTOR ANTAGONISTS

Authors
MILLS SG MACCOSS M UNDERWOOD D SHAH SK FINKE PE MILLER DJ BUDHU RJ CASCIERI MA SADOWSKI S STRADER CD
Citation
Sg. Mills et al., 1,2,3-TRISUBSTITUTED CYCLOHEXYL SUBSTANCE-P ANTAGONISTS - SIGNIFICANCE OF THE RING NITROGEN IN PIPERIDINE-BASED NK-1 RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 5(13), 1995, pp. 1345-1350
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
13
Year of publication
1995
Pages
1345 - 1350
Database
ISI
SICI code
0960-894X(1995)5:13<1345:1CSA-S>2.0.ZU;2-A
Abstract
A stereocontrolled synthesis of 1-benzyloxy-2-phenylcyclohexane deriva tives containing polar substituents at C3 is described. These compound s, designed to test the role of the ring nitrogen in a related series of potent piperidine-based substance P antagonists, show similar NK-1 receptor affinity, indicating that the nitrogen may serve a largely st ructural role in N-substituted piperidine antagonists.