Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration

被引：5
|
作者：
Sparks, Steven M.
Zhou, Huiqiang
Generaux, Claudia
Harston, Lindsey
Moncol, David
Jayawickreme, Channa
Parham, Janet
Condreay, Patrick
Rimele, Thomas
机构：
[1] GlaxoSmithKline, Enteroendocrine Discovery Performance Unit, 5 Moore Dr, Res Triangle Pk, NC 27709 USA
[2] GlaxoSmithKline, Platform Technol & Sci, 5 Moore Dr, Res Triangle Pk, NC 27709 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 08期
关键词：
Scavenger receptor class B type I; SR-BI inhibitor; Nonabsorbed SR-BI inhibitor; Intestinal SR-BI; HIGHLY POTENT; CHOLESTEROL; DISCOVERY; ENTRY; ABSORPTION; TRANSPORT; LIPIDS; CD36;
D O I：
10.1016/j.bmcl.2016.03.025
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The identification of a low-permeability scavenger receptor BI (SR-BI) inhibitor starting from the ITX-5061 template is described. Structure-activity and structure-permeability relationships were assessed for analogs leading to the identification of compound 8 as a potent and nonabsorbable SR-BI inhibitor. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1901 / 1904
页数：4
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