172733-06-1Relevant articles and documents
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.
The first potent inhibitor of mammalian group X secreted phospholipase A2: Elucidation of sites for enhanced binding
Smart, Brian P.,Oslund, Rob C.,Walsh, Laura A.,Gelb, Michael H.
, p. 2858 - 2860 (2007/10/03)
Using the X-ray structure of human group X secreted phospholipase A 2 (hGX), we carried out structure-based design of indole-based inhibitors and prepared the compounds using a new synthetic route. The most potent compound inhibited hGX and the mouse orthologue with an IC50 of 75 nM. This compound is the most potent hGX inhibitor reported to date and was also found to inhibit a subset of the other mouse and human SPLA 2S.
Novel sPLA2 inhibitors
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Page/Page column 22, (2010/11/30)
A class of novel indole is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
