1031414-84-2Relevant academic research and scientific papers
Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2
Corbett, Jeffrey W.,Freeman-Cook, Kevin D.,Elliott, Richard,Vajdos, Felix,Rajamohan, Francis,Kohls, Darcy,Marr, Eric,Zhang, Hailong,Tong, Liang,Tu, Meihua,Murdande, Sharad,Doran, Shawn D.,Houser, Janet A.,Song, Wei,Jones, Christopher J.,Coffey, Steven B.,Buzon, Leanne,Minich, Martha L.,Dirico, Kenneth J.,Tapley, Susan,Kirk McPherson,Sugarman, Eliot,James Harwood Jr.,Esler, William
scheme or table, p. 2383 - 2388 (2010/08/03)
Screening Pfizer's compound library resulted in the identification of weak acetyl-CoA carboxylase inhibitors, from which were obtained rACC1 CT-domain co-crystal structures. Utilizing HTS hits and structure-based drug discovery, a more rigid inhibitor was designed and led to the discovery of sub-micromolar, spirochromanone non-specific ACC inhibitors. Low nanomolar, non-specific ACC-isozyme inhibitors that exhibited good rat pharmacokinetics were obtained from this chemotype.
SPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS
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Page/Page column 62; 65, (2008/12/06)
The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating mammals suffering from the condition of being overweight.
