Novel non-peptidic neuropeptide Y Y2 receptor antagonists. 2004

Jill A Jablonowski, and Wenying Chai, and Xiaobing Li, and Dale A Rudolph, and William V Murray, and Mark A Youngman, and Scott L Dax, and Diane Nepomuceno, and Pascal Bonaventure, and Timothy W Lovenberg, and Nicholas I Carruthers
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. jjablono@prdus.jnj.com

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.

UI MeSH Term Description Entries
D010880 Piperidines A family of hexahydropyridines.
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D017476 Receptors, Neuropeptide Y Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells. Neuropeptide Y Receptors,Neuropeptide Y Receptor,Receptor, Neuropeptide Y

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