Synthesis and SAR of potent LXR agonists containing an indole pharmacophore期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Synthesis and SAR of potent LXR agonists containing an indole pharmacophore

Authors:	David G. Washburn Tram H. Hoang Nino Campobasso Angela Smallwood Derek J. Parks Christine L. Webb Kelly A. Frank Melanie Nord Chaya Duraiswami Christopher Evans Michael Jaye Scott K. Thompson

Affiliation:	1. Department of Chemistry, Molecular Discovery Research, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, USA;2. Department of Biology, Molecular Discovery Research, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, USA;3. Department of Drug Metabolism and Pharmacokinetics, Molecular Discovery Research, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, USA;4. Metabolic Pathways Centre for Excellence in Drug Discovery and Computational and Structural Chemistry, Molecular Discovery Research, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, USA;5. Molecular Discovery Research GlaxoSmithKline, Research Triangle Park, NC 27709, USA

Abstract:	A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRα will be disclosed.

Keywords:
本文献已被 ScienceDirect 等数据库收录！