NK1 antagonists based on seven membered lactam scaffolds.
A new class of high affinity hNK1R antagonists based on seven-membered ring cores has been identified. This series, with relatively simple, compact structures, includes compounds with high affinity, good selectivity, and promising in vivo properties.
Elliott
Jason M
JM
Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. jason@elliottj25.fsnet.co.uk
Carlson
Emma J
EJ
Chicchi
Gary G
GG
Dirat
Olivier
O
Dominguez
Maria
M
Gerhard
Ute
U
Jelley
Richard
R
Jones
A Brian
AB
Kurtz
Marc M
MM
Tsao
Kwei lan
Kl
Wheeldon
Alan
A
D002460:Cell Line; D006801:Humans; D007769:Lactams / Q000737:chemistry*; D015394:Molecular Structure; D064729:Neurokinin-1 Receptor Antagonists; D013329:Structure-Activity Relationship
D007769:Lactams; D064729:Neurokinin-1 Receptor Antagonists