Cameron J Smith,
Amjad Ali,
Milton L Hammond, Hong Li,
Zhijian Lu,
Joann Napolitano,
Gayle E Taylor,
Christopher F Thompson,
Matt S Anderson,
Ying Chen, [......],
Carl P Sparrow,
Samuel D Wright,
Anne-Marie Cumiskey,
Melanie Latham,
Laurence B Peterson,
Ray Rosa,
James V Pivnichny,
Xinchun Tong,
Suoyu S Xu,
Peter J Sinclair
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ABSTRACT: The development of the structure-activity studies leading to the discovery of anacetrapib is described. These studies focused on varying the substitution of the oxazolidinone ring of the 5-aryloxazolidinone system. Specifically, it was found that substitution of the 4-position with a methyl group with the cis-stereochemistry relative to the 5-aryl group afforded compounds with increased cholesteryl ester transfer protein (CETP) inhibition potency and a robust in vivo effect on increasing HDL-C levels in transgenic mice expressing cynomolgus monkey CETP.
Journal of Medicinal Chemistry 06/2011; 54(13):4880-95. · 4.80 Impact Factor
