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Bioorg Med Chem Lett. 2012 Jan 1;22(1):334-8. doi: 10.1016/j.bmcl.2011.11.002. Epub 2011 Nov 9.

Discovery of cyclic amine-substituted benzoic acids as PPARα agonists.

Author information

  • 1Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd, 2399-1, Nogi, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan. masahiro.nomura@mb.kyorin-pharm.co.jp

Abstract

A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPARα agonist activity. Strucure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthyazole-5-carboxamido]piperidin-1-yl]benzoic acid (S)-4f (KRP-105) as a potent and high subtype-selective human PPARα agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides.

PMID:
22133631
DOI:
10.1016/j.bmcl.2011.11.002
[PubMed - indexed for MEDLINE]
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