| Literature DB >> 19482480 |
Steven J Kirincich1, Jason Xiang, Neal Green, Steve Tam, Hui Y Yang, Jaechul Shim, Marina W H Shen, James D Clark, John C McKew.
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.Entities:
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Year: 2009 PMID： 19482480 DOI： 10.1016/j.bmc.2009.05.027
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641