SAR studies: Designing potent and selective LXR agonists

Bioorganic & Medicinal Chemistry Letters
2006.0

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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