1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor
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DOI：
10.1016/s0960-894x(01)00343-2
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发表时间：
2001-07-23
影响因子：
2.7
通讯作者：
Austin, N
中科院分区：
文献类型：
--
作者：
Porter, RA;Chan, WN;Austin, N
该通讯报告了第一个食欲素-1受体拮抗剂系列1-芳基-3-喹啉-4-基和1-芳基-3-萘啶-4-基脲的SAR。这些化合物之一，31（5 B-334867），对食欲素-1受体、血脑屏障渗透性具有优异的选择性，并在ip给药后显示出体内活性。(C)2001爱思唯尔科技有限公司版权所有。
This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quifiolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (5B-334867), has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing. (C) 2001 Elsevier Science Ltd. All rights reserved.