875446-61-0Relevant articles and documents
SAR studies on the central phenyl ring of substituted biphenyl oxazolidinone-potent CETP inhibitors
Lu, Zhijian,Chen, Yi-Heng,Napolitano, Joann B.,Taylor, Gayle,Ali, Amjad,Hammond, Milton L.,Deng, Qiaolin,Tan, Eugene,Tong, Xinchun,Xu, Suoyu S.,Latham, Melanie J.,Peterson, Laurence B.,Anderson, Matt S.,Eveland, Suzanne S.,Guo, Qiu,Hyland, Sheryl A.,Milot, Denise P.,Chen, Ying,Sparrow, Carl P.,Wright, Samuel D.,Sinclair, Peter J.
scheme or table, p. 199 - 203 (2012/02/16)
SAR studies of the substitution effect on the central phenyl ring of the biphenyl scaffold were carried out using anacetrapib (9a) as the benchmark. The results revealed that the new analogs with substitutions to replace trifluoromethyl (9a) had a significant impact on CETP inhibition in vitro. In fact, analogs with some small groups were as potent or more potent than the CF3 derivative for CETP inhibition. Five of these new analogs raised HDL-C significantly (>20 mg/dL). None of them however was better than anacetrapib in vivo. The synthesis and biological evaluation of these CETP inhibitors are described.
CETP INHIBITORS
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Page/Page column 87, (2010/10/19)
Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalky substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalky substituent connected directly to the ring or attached to the ring through a -CH2-.
