Jablonowski Jill A, Chai Wenying, Li Xiaobing, Rudolph Dale A, Murray William V, Youngman Mark A, Dax Scott L, Nepomuceno Diane, Bonaventure Pascal, Lovenberg Timothy W, Carruthers Nicholas I
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1239-42. doi: 10.1016/j.bmcl.2003.12.057.
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.
通过对哌啶基吲哚啉肉桂酰胺高通量筛选先导化合物的构效关系(SAR)研究,已合成出首个强效、非肽、低分子量的选择性神经肽Y Y2(NPY Y2)拮抗剂。本文讨论了围绕哌啶基、吲哚啉基和肉桂基部分的构效关系研究。