Novel non-peptidic neuropeptide Y Y2 receptor antagonists

Jill A Jablonowski; Wenying Chai; Xiaobing Li; Dale A Rudolph; William V Murray; Mark A Youngman; Scott L Dax; Diane Nepomuceno; Pascal Bonaventure; Timothy W Lovenberg; Nicholas I Carruthers

doi:10.1016/j.bmcl.2003.12.057

Novel non-peptidic neuropeptide Y Y2 receptor antagonists

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1239-42. doi: 10.1016/j.bmcl.2003.12.057.

Authors

Jill A Jablonowski¹, Wenying Chai, Xiaobing Li, Dale A Rudolph, William V Murray, Mark A Youngman, Scott L Dax, Diane Nepomuceno, Pascal Bonaventure, Timothy W Lovenberg, Nicholas I Carruthers

Affiliation

¹ Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. jjablono@prdus.jnj.com

PMID: 14980673
DOI: 10.1016/j.bmcl.2003.12.057

Abstract

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.

MeSH terms

Humans
Piperidines / chemistry*
Piperidines / metabolism
Piperidines / pharmacology
Protein Binding
Receptors, Neuropeptide Y / antagonists & inhibitors*
Receptors, Neuropeptide Y / metabolism

Substances

Piperidines
Receptors, Neuropeptide Y
neuropeptide Y2 receptor