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Bioorg Med Chem Lett. 2012 Jan 1;22(1):199-203. doi: 10.1016/j.bmcl.2011.11.039. Epub 2011 Nov 16.

SAR studies on the central phenyl ring of substituted biphenyl oxazolidinone-potent CETP inhibitors.

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1
Department of Medicinal Chemistry, Merck Sharp & Dohme Corp., PO Box 2000, Rahway, NJ 07065, USA. zhijian_lu@merck.com

Abstract

SAR studies of the substitution effect on the central phenyl ring of the biphenyl scaffold were carried out using anacetrapib (9a) as the benchmark. The results revealed that the new analogs with substitutions to replace trifluoromethyl (9a) had a significant impact on CETP inhibition in vitro. In fact, analogs with some small groups were as potent or more potent than the CF(3) derivative for CETP inhibition. Five of these new analogs raised HDL-C significantly (>20mg/dL). None of them however was better than anacetrapib in vivo. The synthesis and biological evaluation of these CETP inhibitors are described.

PMID:
22142541
DOI:
10.1016/j.bmcl.2011.11.039
[Indexed for MEDLINE]
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