Novel highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulators with pharmacokinetic properties suitable for once-daily oral dosing. Issue 23 (1st December 2017)

• Record Type: Journal Article
• Authors: Lagu, Bharat; Kluge, Arthur F.; Fredenburg, Ross A.; Tozzo, Effie; Senaiar, Ramesh S.; Jaleel, Mahaboobi; Panigrahi, Sunil K.; Tiwari, Nirbhay K.; Krishnamurthy, Narasimha R.; Takahashi, Taisuke; Patane, Michael A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 23(2017)
• Page Start: 5230
• Page End: 5234
• Publication Date: 2017-12-01
• Subjects: PPARδ modulator -- GW501516 -- Plasma exposure -- Ligand binding domain -- X-ray structure; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.10.037
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Optimization of benzamide PPARδ modulator1 led to ( E )-6-(2-((4-(furan-2-yl)- N -methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18 ), a potent selective PPARδ modulator with significantly improved exposure in multiple species following oral administration.