42018-09-7Relevant articles and documents
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists
Makadia, Pankaj,Shah, Shailesh R.,Pingali, Harikishore,Zaware, Pandurang,Patel, Darshit,Pola, Suresh,Thube, Baban,Priyadarshini, Priyanka,Suthar, Dinesh,Shah, Maanan,Giri, Suresh,Trivedi, Chitrang,Jain, Mukul,Patel, Pankaj,Bahekar, Rajesh
experimental part, p. 771 - 782 (2011/03/18)
A novel series of thaizole and oxazole containing phenoxy acetic acid derivatives is reported as PPAR-pan agonists. Incorporation of structurally constrained oxime-ether based linker in the chemotype of a potent PPARδ selective agonist GW-501516 was adapted as designing strategy. In vitro, selected test compounds 12a, 12c, 17a and 18a showed PPAR-pan agonists activities and among these four compounds tested, 12a emerged as highly potent and efficacious compound, while 17a exhibited moderate and balanced PPAR-pan agonistic activity. In vivo, selected test compounds 12a and 17a exhibited significant anti-hyperglycemic and anti-hyperlipidemic activities in relevant animal models. These results support our hypothesis that the introduction of structurally constrained oxime-ether linker between lipophilic tail and acidic head plays an important role in modulating subtype selectivity and subsequently led to the discovery of potent PPAR-pan agonists.
GPR120 RECEPTOR AGONISTS AND USES THEREOF
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Page/Page column 132, (2012/01/06)
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
GPR120 RECEPTOR AGONISTS AND USES THEREOF
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Page/Page column 107, (2010/08/04)
GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.