SAR studies: designing potent and selective LXR agonists

Bioorganic & Medicinal Chemistry Letters
Jason W SzewczykAlan D Adams

Abstract

Counterscreening compounds from a Merck PPAR program discovered lead 1, as a nanomolar LXR/PPAR dual agonist. SAR optimization developed a series of heterocyclic LXR agonists having excellent selectivity over all PPAR isoforms and possessing high LXR affinity and strong in vivo potency.

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Citations

Mar 26, 2011·Journal of Chemical Information and Modeling·Wenxia ZhaoJun Xu
May 21, 2016·Cell Chemical Biology·Ian CookThomas S Leyh
Feb 9, 2017·Bioorganic & Medicinal Chemistry Letters·Pascal HeitelDaniel Merk
Jan 12, 2010·Molecular Informatics·Morena SpreaficoAngelo Vedani
May 17, 2014·Journal of Medicinal Chemistry·Colin M TiceSuresh B Singh
Apr 12, 2012·Journal of Chemical Information and Modeling·Susanne von GrafensteinDaniela Schuster

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