2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety

Compound 47 was found to be a potent inhibitor of CETP and had an IC 50 of 28 nM. 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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010, Vol.20 (1), p.346-349
Main Authors: Smith, Cameron J., Ali, Amjad, Chen, Liya, Hammond, Milton L., Anderson, Matt S., Chen, Ying, Eveland, Suzanne S., Guo, Qiu, Hyland, Sheryl A., Milot, Denise P., Sparrow, Carl P., Wright, Samuel D., Sinclair, Peter J.
Format: Article
Language:eng
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HDL
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Summary:Compound 47 was found to be a potent inhibitor of CETP and had an IC 50 of 28 nM. 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 IC 50 of 28 nM.
ISSN:0960-894X
1464-3405