1.
Bioorg Med Chem Lett
; 12(13): 1755-8, 2002 Jul 08.
Article
in English
| MEDLINE
| ID: mdl-12067554
ABSTRACT
A series of novel 4,4-disubstituted cyclohexylamine based NK(1) antagonists is described. The effect of changes to the C(1)-C(4) relative stereochemistry on the cyclohexane ring and replacements for the flexible linker are discussed, leading to the identification of compounds with high affinity and good in vivo duration of action.
Subject(s)
Cyclohexylamines/chemical synthesis , Cyclohexylamines/pharmacology , Neurokinin-1 Receptor Antagonists , Animals , Binding Sites , CHO Cells , Central Nervous System/drug effects , Central Nervous System/metabolism , Cricetinae , Cyclohexylamines/pharmacokinetics , Gerbillinae , Inhibitory Concentration 50 , Molecular Conformation , Radioligand Assay , Receptors, Neurokinin-1/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 12(13): 1759-62, 2002 Jul 08.
Article
in English
| MEDLINE
| ID: mdl-12067555
ABSTRACT
A series of novel 4,4-disubstituted cyclohexylamines as NK(1) receptor antagonists is described: modifications to the amine moiety retain NK(1) receptor binding affinity whilst disrupting I(Kr) affinity.
