Synthesis and SAR of potent LXR agonists containing an indole pharmacophore

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

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. This manuscript will describe optimization of this series of LXR agonists using a structure-based design strategy. In addition, the SAR of this novel series and a crystal structure of a selected ligand bound to the LXRα LBD will be disclosed.

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关键词

LXR,Liver X receptors,Nuclear hormone receptors,Pulmonary inflammation,Diabetes,Atherosclerosis

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