title: Discovery of a series of potent, orally active α,α-disubstituted piperidine NK(1) antagonists.
abstract: Modification of prototype NK(1) antagonist 2 resulted in the synthesis of a series of simple amides 6 and retroamides 9. These compounds were shown to be potent and orally active NK(1) antagonists.
authors.affiliation: Chemical Research Department, Merck Research Laboratories, Kenilworth, NJ 07033, USA. dong.xiao@merck.com
authors.forename: Dong
authors.initials: D
authors.lastname: Xiao
authors.forename: Cheng
authors.initials: C
authors.lastname: Wang
authors.forename: Anandan
authors.initials: A
authors.lastname: Palani
authors.forename: Hon-Chung
authors.initials: HC
authors.lastname: Tsui
authors.forename: Gregory
authors.initials: G
authors.lastname: Reichard
authors.forename: Sunil
authors.initials: S
authors.lastname: Paliwal
authors.forename: Neng-Yang
authors.initials: NY
authors.lastname: Shih
authors.forename: Robert
authors.initials: R
authors.lastname: Aslanian
authors.forename: Ruth
authors.initials: R
authors.lastname: Duffy
authors.forename: Jean
authors.initials: J
authors.lastname: Lachowicz
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Varty
authors.forename: Cynthia
authors.initials: C
authors.lastname: Morgan
authors.forename: Fei
authors.initials: F
authors.lastname: Liu
authors.forename: Amin
authors.initials: A
authors.lastname: Nomeir
mesh_terms: D000818:Animals; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D005849:Gerbillinae; D006207:Half-Life; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines