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.
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
Jason M
JM
Elliott
Emma J
EJ
Carlson
Gary G
GG
Chicchi
Olivier
O
Dirat
Maria
M
Dominguez
Ute
U
Gerhard
Richard
R
Jelley
A Brian
AB
Jones
Marc M
MM
Kurtz
Kwei lan
Kl
Tsao
Alan
A
Wheeldon
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