Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Oslund, Rob C.¹  Cermak, Nathan¹  Verlinde, Christophe L. M. J.²  Gelb, Michael H.^1,2 

[1] Univ Washington, Dept Chem, Seattle, WA 98195 USA

[2] Univ Washington, Dept Biochem, Seattle, WA 98195 USA

关键词: eicosanoids;    lipid mediators;    inflammation;    structure-based drug design;    phospholipases;   

DOI  :  10.1016/j.bmcl.2008.09.041

来源: Elsevier

【 摘 要 】

Simplified analogs of YM-26734, a known inhibitor of secreted phospholipase A(2) (sPLA(2)) group IIA, were synthesized and found to also display potent inhibition at low nanomolar concentrations. Analogs were based on the didodecanoylphloroglucinol portion of YM-26734 which contains the predicted active site calcium binding group. (C) 2008 Elsevier Ltd. All rights reserved.

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