Benzhydrylquinazolinediones: Novel cytosolic phospholipase A 2 α inhibitors with improved physicochemical properties

SJ Kirincich, J Xiang, N Green, S Tam, HY Yang…

Index: Kirincich, Steven J.; Xiang, Jason; Green, Neal; Tam, Steve; Yang, Hui Y.; Shim, Jaechul; Shen, Marina W.H.; Clark, James D.; McKew, John C. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 13 p. 4383 - 4405

Full Text: HTML

Citation Number: 23

Abstract

The synthesis and optimization of a class of trisubstituted quinazoline-2, 4 (1H, 3H)-dione cPLA2α 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 ...

Related Articles:

Highly reactive, general and long-lived catalysts for palladium-catalyzed amination of heteroaryl and aryl chlorides, bromides, and iodides: scope and structure– …

[Shen, Qilong; Ogata, Tokutaro; Hartwig, John F. Journal of the American Chemical Society, 2008 , vol. 130, # 20 p. 6586 - 6596]

Reinvestigating Raney nickel mediated selective alkylation of amines with alcohols via hydrogen autotransfer methodology

[Mehta, Astha; Thaker; Londhe; Nandan, Santosh R. Applied Catalysis A: General, 2014 , vol. 478, p. 241 - 251]

A practical method for preparation of 4-hydroxyquinolinone esters

[Beutner, Gregory L.; Kuethe, Jeffrey T.; Yasuda, Nobuyoshi Journal of Organic Chemistry, 2007 , vol. 72, # 18 p. 7058 - 7061]

A practical method for preparation of 4-hydroxyquinolinone esters

[Beutner, Gregory L.; Kuethe, Jeffrey T.; Yasuda, Nobuyoshi Journal of Organic Chemistry, 2007 , vol. 72, # 18 p. 7058 - 7061]

A practical method for preparation of 4-hydroxyquinolinone esters

[Beutner, Gregory L.; Kuethe, Jeffrey T.; Yasuda, Nobuyoshi Journal of Organic Chemistry, 2007 , vol. 72, # 18 p. 7058 - 7061]

More Articles...