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Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties.

Abstract：

:The synthesis and optimization of a class of trisubstituted quinazoline-2,4(1H,3H)-dione cPLA(2)alpha inhibitors are described. Utilizing pharmacophores that were found to be important in our indole series, we discovered inhibitors with reduced lipophilicity and improved aqueous solubility. These compounds are active in whole blood assays, and cell-based assay results indicate that prevention of arachidonic acid release arises from selective cPLA(2)alpha inhibition.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kirincich SJ,Xiang J,Green N,Tam S,Yang HY,Shim J,Shen MW,Clark JD,McKew JC

doi

10.1016/j.bmc.2009.05.027

subject

Has Abstract

pub_date

2009-07-01 00:00:00

pages

4383-405

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00479-9

journal_volume

17

pub_type

杂志文章

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