2. Academic Validation
  3. SAR studies: designing potent and selective LXR agonists

SAR studies: designing potent and selective LXR agonists

  • Bioorg Med Chem Lett. 2006 Jun 1;16(11):3055-60. doi: 10.1016/j.bmcl.2006.02.050.
Jason W Szewczyk 1,  Shaei Huang,  Jayne Chin,  Jenny Tian,  Lyndon Mitnaul,  Raymond L Rosa,  Larry Peterson,  Carl P Sparrow,  Alan D Adams
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. [email protected]
PMID: 16529931 DOI: 10.1016/j.bmcl.2006.02.050
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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