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2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety |
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| Authors: | Cameron J Smith Amjad Ali Liya Chen Milton L Hammond Matt S Anderson Ying Chen Suzanne S Eveland Qiu Guo Sheryl A Hyland Denise P Milot Carl P Sparrow Samuel D Wright Peter J Sinclair |
| Institution: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway NJ 07065, United States;2. Department of Cardiovascular Diseases, Merck Research Laboratories, Rahway NJ 07065, United States |
| Abstract: | A series of 2-arylbenzoxazole inhibitors of the cholesterol ester transfer protein (CETP) is described. Structure–activity studies focused on variation of the substitution of the benzoxazole moiety. Substitution at the 5- and 7-positions of the benzoxazole moiety was found to be beneficial for CETP inhibition. Compound 47 was found to be the most potent inhibitor in this series and inhibited CETP with an IC50 of 28 nM. |
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