Porter R A, Chan W N, Coulton S, Johns A, Hadley M S, Widdowson K, Jerman J C, Brough S J, Coldwell M, Smart D, Jewitt F, Jeffrey P, Austin N
GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park North, Third Avenue, Harlow, CM19 5AW, Essex, UK.
Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10. doi: 10.1016/s0960-894x(01)00343-2.
This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quinolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (SB-334867), has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing.
本通讯报道了1-芳基-3-喹啉-4-基脲和1-芳基-3-吡啶并[2,3-b]吡啶-4-基脲的首个食欲素-1受体拮抗剂系列的SARs。其中一种化合物31（SB-334867）对食欲素-1受体具有优异的选择性、血脑屏障通透性，并且腹腔注射给药后显示出体内活性。
