Synthesis and identification of [1, 2, 4] thiadiazole derivatives as a new series of potent and orally active dual agonists of peroxisome proliferator-activated receptors α …

…, Y Zhang, A Wang, E Sieber-McMaster…

Index: Shen, Lan; Zhang, Yan; Wang, Aihua; Sieber-McMaster, Ellen; Chen, Xiaoli; Pelton, Patricia; Xu, Jun Z.; Yang, Maria; Zhu, Peifang; Zhou, Lubing; Reuman, Michael; Hu, Zhiyong; Russell, Ronald; Gibbs, Alan C.; Ross, Hamish; Demarest, Keith; Murray, William V.; Kuo, Gee-Hong Journal of Medicinal Chemistry, 2007 , vol. 50, # 16 p. 3954 - 3963

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Citation Number: 37

Abstract

Cardiovascular disease is the most common cause of morbidity and mortality in developed nations. To effectively target dyslipidemia to reduce the risk of cardiovascular disease, it may be beneficial to activate the peroxisome proliferator-activated receptors (PPARs) PPARα and PPARδ simultaneously through a single molecule. Replacement of the methylthiazole of 5 (the PPARδ selective agonist) with [1, 2, 4] thiadiazole gave compound 13, which ...