Indanylacetic acids as PPAR-δ activator insulin sensitizers

• Published in: Bioorganic & medicinal chemistry letters Vol. 17; no. 15; pp. 4369 - 4373
• Main Authors: Wickens, Philip, Zhang, Chengzhi, Ma, Xin, Zhao, Qian, Amatruda, John, Bullock, William, Burns, Michael, Cantin, Louis-David, Chuang, Chih-Yuan, Claus, Thomas, Dai, Miao, Dela Cruz, Fernando, Dickson, David, Ehrgott, Frederick J., Fan, Dongping, Heald, Sarah, Hentemann, Martin, Iwuagwu, Christiana I., Johnson, Jeffrey S., Kumarasinghe, Ellalahewage, Ladner, David, Lavoie, Rico, Liang, Sidney, Livingston, James N., Lowe, Derek, Magnuson, Steve, Mannelly, Gretchen, Mugge, Ingo, Ogutu, Herbert, Pleasic-Williams, Susan, Schoenleber, Robert W., Shapiro, Jeff, Shelekhin, Tatiana, Sweet, Laurel, Town, Christopher, Tsutsumi, Manami
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.08.2007; Elsevier
• Subjects: Biological and medical sciences; Fluorescence Resonance Energy Transfer; General and cellular metabolism. Vitamins; Indane acetic acids; Insulin Resistance; Insulin sensitizer; Medical sciences; Pharmacology. Drug treatments; PPAR; PPAR delta - agonists; Structure-Activity Relationship; PPAR; Insulin sensitizer; Indane acetic acids; Pancreatic hormone; Nuclear receptor; Indan derivatives; Ligand; PPAR-β receptor; Selectivity; Acetic acid derivative; In vitro; Insulin; Protein hormone; In vivo; Structure activity relation; Activator; Animal; Chemical synthesis; Oxazole derivatives; Peroxisome proliferator activated receptor; Sensitizer; Biological receptor
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2007.03.057

A novel series of indane acetic acid molecules are insulin sensitizers and have selectivity for PPAR-δ agonist activity over PPAR-α. A series of indane acetic acid derivatives were prepared which show a spectrum of activity as insulin sensitizers and PPAR-α and PPAR-δ ligands. In vivo data are presented for insulin sensitizers with selectivity for PPAR-δ over PPAR-α.