SAR studies: designing potent and selective LXR agonists |
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| Authors: | Szewczyk Jason W Huang Shaei Chin Jayne Tian Jenny Mitnaul Lyndon Rosa Raymond L Peterson Larry Sparrow Carl P Adams Alan D |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. jason_szewczyk@merck.com |
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| 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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