2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.
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.
Cooper
L C
LC
Department of Medicinal Chemistry, The Neuroscience Research Centre, Harlow, Essex, UK. laura_cooper@merck.com
Chicchi
G G
GG
Dinnell
K
K
Elliott
J M
JM
Hollingworth
G J
GJ
Kurtz
M M
MM
Locker
K L
KL
Morrison
D
D
Shaw
D E
DE
Tsao
K L
KL
Watt
A P
AP
Williams
A R
AR
Swain
C J
CJ
D000818:Animals; D001522:Behavior, Animal; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry; D016466:CHO Cells; D006224:Cricetinae; D005849:Gerbillinae; D007202:Indicators and Reagents; D007211:Indoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D064729:Neurokinin-1 Receptor Antagonists; D051381:Rats; D013329:Structure-Activity Relationship; D013373:Substance P / Q000378:metabolism
D007202:Indicators and Reagents; D007211:Indoles; D064729:Neurokinin-1 Receptor Antagonists; D013373:Substance P