High affinity phenylglycinol-based NK1 receptor antagonists.
Heterocyclic replacements for the carboxamido group of the previously disclosed phenylglycinol-based human NK1 (hNK1) receptor antagonists have been investigated, ultimately leading to acyclic compounds with sub-nanomolar affinity for the hNK1 receptor.
Owens
A P
AP
Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, Harlow, Essex, U.K. andrew_owens@merck.com
Harrison
T
T
Moseley
J D
JD
Swain
C J
CJ
Sadowski
S
S
Cascieri
M A
MA
D004983:Ethanolamines; D005998:Glycine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D064729:Neurokinin-1 Receptor Antagonists; D013329:Structure-Activity Relationship
D004983:Ethanolamines; D064729:Neurokinin-1 Receptor Antagonists; C005332:N-phenylethanolamine; D005998:Glycine