1353776-75-6Relevant academic research and scientific papers
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase
Bourbeau, Matthew P.,Siegmund, Aaron,Allen, John G.,Shu, Hong,Fotsch, Christopher,Bartberger, Michael D.,Kim, Ki-Won,Komorowski, Renee,Graham, Melissa,Busby, James,Wang, Minghan,Meyer, James,Xu, Yang,Salyers, Kevin,Fielden, Mark,Véniant, Murielle M.,Gu, Wei
supporting information, p. 10132 - 10141 (2014/01/17)
Acetyl-CoA carboxylase (ACC) is a target of interest for the treatment of metabolic syndrome. Starting from a biphenyloxadiazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed. Initial pharmacokinetic liabilities of the piperazine oxadiazoles were overcome by blocking predicted sites of metabolism, resulting in compounds with suitable properties for further in vivo studies. Compound 26 was shown to inhibit malonyl-CoA production in an in vivo pharmacodynamic assay and was advanced to a long-term efficacy study. Prolonged dosing with compound 26 resulted in impaired glucose tolerance in diet-induced obese (DIO) C57BL6 mice, an unexpected finding.
NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Page/Page column 49, (2012/06/30)
The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
