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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Published in: | Bioorganic & medicinal chemistry letters 2010, Vol.20 (1), p.346-349 |
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Main Authors: | , , , , , , , , , , , , |
Format: | Article |
Language: | eng |
Subjects: | |
Online Access: | Get full text |
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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. |
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ISSN: | 0960-894X 1464-3405 |