L-tryptophan urea amides as NK1/NK2 dual antagonists.
We report that a systematic modification of an NK1 receptor selective antagonist resulted in the identification of novel compounds, 4c and 4d, with high affinity for both NK1 and NK2 receptors.
Qi
H
H
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Shah
S K
SK
Cascieri
M A
MA
Sadowski
S J
SJ
MaCcoss
M
M
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D015394:Molecular Structure; D064729:Neurokinin-1 Receptor Antagonists; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D014364:Tryptophan / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000577:Amides; D007202:Indicators and Reagents; D064729:Neurokinin-1 Receptor Antagonists; D018041:Receptors, Neurokinin-2; D011994:Recombinant Proteins; D014364:Tryptophan