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

页码：1901 / 1904

页数：4

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