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Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors.

Abstract：

:2,3-Dihydro-3,8-diphenylbenzo[1,4]oxazines were identified as a new class of potent cholesteryl ester transfer protein inhibitors. The most potent compound 6a (IC50=26 nM) possessed a favorable pharmacokinetic profile with good oral bioavailability in rat (F=53%) and long human liver microsome stability (t(1/2)=62 min). It increased HDL-C in human CETP transgenic mice and high-fat fed hamsters. The structure and activity relationship of this series will be described in this Letter.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wang A,Prouty CP,Pelton PD,Yong M,Demarest KT,Murray WV,Kuo GH

doi

10.1016/j.bmcl.2009.12.096

subject

Has Abstract

pub_date

2010-02-15 00:00:00

pages

1432-5

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01819-8

journal_volume

20

pub_type

杂志文章

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