1.
Bioorg Med Chem Lett
; 11(9): 1233-6, 2001 May 07.
Article
in English
| MEDLINE
| ID: mdl-11354384
ABSTRACT
The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the indole substitution.
Subject(s)
Indoles/chemical synthesis , Indoles/pharmacology , Neurokinin-1 Receptor Antagonists , Animals , Behavior, Animal , Binding, Competitive/drug effects , Brain Chemistry , CHO Cells , Cricetinae , Gerbillinae , Indicators and Reagents , Indoles/pharmacokinetics , Rats , Structure-Activity Relationship , Substance P/metabolism
2.
Bioorg Med Chem Lett
; 11(9): 1237-40, 2001 May 07.
Article
in English
| MEDLINE
| ID: mdl-11354385
ABSTRACT
Novel 2-aryl indole hNK1 receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK1 receptor binding affinity and good brain penetration (e.g., 9d) were synthesised.