Document Report Card

ID: ALA1155819

Journal: J Med Chem

Title: Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.

Authors: Oslund RC, Cermak N, Gelb MH.

Abstract: We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, we prepared a highly potent and selective indole-based inhibitor of this enzyme. Also, we report human and mouse group IIA and IIE specific inhibitors and a substituted 6,7-benzoindole that inhibits nearly all human and mouse sPLA2s in the low nanomolar range.

CiteXplore: 18605714

DOI: 10.1021/jm800422v