177556-97-7Relevant academic research and scientific papers
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2
Oslund, Rob C.,Cermak, Nathan,Gelb, Michael H.
supporting information; experimental part, p. 4708 - 4714 (2009/06/06)
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.
Indolizine SPLA2inhibitors
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Page/Page column 60, (2010/11/30)
A class of novel indolizine-1-functional compounds and indolizine-3-functional compounds is disclosed together with the use of such indolizine compounds for inhibiting sPLA2mediated release of fatty acids for treatment of conditions such as septic shock. The compounds are indolizine-1-acetamides, indolizine-1-acetic acid hydrazides, indolizine-1-glyoxylamides, indolizine-3-acetamides, indolizine-3-acetic acid hydraxides, and indolizine-3-glyoxylasides.
