Novel non-peptidic neuropeptide Y Y2 receptor antagonists.
Through SAR studies of a piperidinylindoline cinnamide HTS lead, the first potent, non-peptide, low molecular weight selective Neuropeptide Y Y2 (NPY Y2) antagonists have been synthesized. The SAR studies around the piperidinyl, the indolinyl, and the cinnamyl moieties are discussed.
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. jjablono@prdus.jnj.com
Jill A
JA
Jablonowski
Wenying
W
Chai
Xiaobing
X
Li
Dale A
DA
Rudolph
William V
WV
Murray
Mark A
MA
Youngman
Scott L
SL
Dax
Diane
D
Nepomuceno
Pascal
P
Bonaventure
Timothy W
TW
Lovenberg
Nicholas I
NI
Carruthers
D006801:Humans; D010880:Piperidines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D011485:Protein Binding; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism
D010880:Piperidines; D017476:Receptors, Neuropeptide Y; C095889:neuropeptide Y2 receptor