Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.
Solution-phase, parallel-synthesis techniques were used to optimize a series of nonbasic NK-1 antagonists, resulting in the identification of (R)-26, an orally bioavailable compound with subnanomolar potency.
Fritz
J E
JE
Lilly Research Laboratories, Eli Lilly and Company, 46285, Indianapolis, IN, USA. j.fritz@lilly.com
Hipskind
P A
PA
Lobb
K L
KL
Nixon
J A
JA
Threlkeld
P G
PG
Gitter
B D
BD
McMillian
C L
CL
Kaldor
S W
SW
D064729:Neurokinin-1 Receptor Antagonists; D013329:Structure-Activity Relationship
D064729:Neurokinin-1 Receptor Antagonists