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Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists |
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| Authors: | Matthews Jay M Chen Xiaoli Cryan Ellen Hlasta Dennis J Rybczynski Philip J Strauss Kim Tang Yuting Xu June Z Yang Maria Zhou Lubing Demarest Keith T |
| Institution: | aDrug Discovery, Johnson & Johnson, East Coast RED, Spring House, PA 19477-0776, USA |
| Abstract: | A series of aminoindane derivatives were synthesized and shown to be potent PPARα agonists. The compounds were obtained as racemates in 12 steps, and tested for PPARα activation and PPARα mediated induction of the HD gene. SAR was developed by variation to the core structure as shown within. Oral bioavailability was demonstrated in a Sprague–Dawley rat, while efficacy to reduce plasma triglycerides and plasma glucose was demonstrated in db/db mice. |
| Keywords: | Aminoindane PPARα agonist Hypolipidemic Hypoglycemic Dyslipidemia |
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