Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) δ agonists

…, GF Filzen, A Geyer, JK Hoffman, G Lu, J Pulaski…

Index: Bratton, Larry D.; Filzen, Gary F.; Geyer, Andrew; Hoffman, Jennifer K.; Lu, Gina; Pulaski, Jim; Trivedi, Bharat K.; Unangst, Paul C.; Xu, Xiangyang Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 13 p. 3624 - 3629

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Citation Number: 8

Abstract

A series of 1, 4-benzyloxybenzylsulfanylaryl carboxylic acids were prepared and their activities for PPAR receptor subtypes (α, δ, and γ) with potential indications for the treatment of dyslipidemia were investigated. Analog 13a displayed the greatest binding affinity (IC50= 10nM) and selectivity (120-fold) for PPARδ over PPARα. Many of the analogs investigated were found to be highly selective for PPARδ and were dependent on the point of ...