2-(4-Carbonylphenyl) benzoxazole inhibitors of CETP: Scaffold design and advancement in HDLc-raising efficacy

…, AM Cumiskey, M Latham, R Rosa, L Peterson…

Index: Sweis, Ramzi F.; Hunt, Julianne A.; Kallashi, Florida; Hammond, Milton L.; Chen, Ying; Eveland, Suzanne S.; Guo, Qiu; Hyland, Sheryl A.; Milot, Denise P.; Cumiskey, Anne-Marie; Latham, Melanie; Rosa, Raymond; Peterson, Larry; Sparrow, Carl P.; Wright, Samuel D.; Anderson, Matt S.; Sinclair, Peter J. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1890 - 1895

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Citation Number: 8

Abstract

The development of 2-phenylbenzoxazoles as inhibitors of cholesteryl ester transfer protein (CETP) is described. Initial efforts aimed at engineering replacements for the aniline substructures in the benchmark molecule. Reversing the connectivity of the central aniline lead to a new class of 2-(4-carbonylphenyl) benzoxazoles. Structure–activity studies at the C- 7 and terminal pyridine ring allowed for the optimization of potency and HDLc-raising ...