- Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2
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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 sPLA 2s in the low nanomolar range.
- Oslund, Rob C.,Cermak, Nathan,Gelb, Michael H.
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supporting information; experimental part
p. 4708 - 4714
(2009/06/06)
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