Journal of medicinal chemistry

Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2

RC Oslund, N Cermak, MH Gelb

Index: Oslund, Rob C.; Cermak, Nathan; Gelb, Michael H. Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4708 - 4714

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Citation Number: 95

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 ...