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Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.

Abstract：

:A low level of high density lipoprotein (HDL) is an independent risk factor for cardiovascular disease. HDL reduces inflammation and plays a central role in reverse cholesterol transport, where cholesterol is removed from peripheral tissues and atherosclerotic plaque. One approach to increase plasma HDL is through inhibition of endothelial lipase (EL). EL hydrolyzes phospholipids in HDL resulting in reduction of plasma HDL. A series of benzothiazole sulfone amides was optimized for EL inhibition potency, lipase selectivity and improved pharmacokinetic profile leading to the identification of Compound 32. Compound 32 was evaluated in a mouse pharmacodynamic model and found to show no effect on HDL cholesterol level despite achieving targeted plasma exposure (Ctrough > 15 fold over mouse plasma EL IC50 over 4 days).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kim SH,Johnson JA,Jiang J,Parkhurst B,Phillips M,Pi Z,Qiao JX,Tora G,Ye Chen A,Liu E,Yin X,Yang R,Zhao L,Taylor DS,Basso M,Behnia K,Onorato J,Chen XQ,Abell LM,Lu H,Locke G,Caporuscio C,Adam LP,Gordon D,Wex

doi

10.1016/j.bmcl.2019.05.048

subject

Has Abstract

pub_date

2019-08-01 00:00:00

pages

1918-1921

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(19)30354-3

journal_volume

29

pub_type

杂志文章

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