164082-80-8Relevant 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.
PHARMACEUTICAL COMPOSITIONS CONTAINING THE PHOSPHOLIPASE INHIBITOR SODIUM 3-(2-AMINO-1,2-DIOXOETHYL)-2-ETHYL-1-PHENYLMETHYL)-1H-INDOL-4-YL]OXY]ACETATE
-
Page/Page column 5, (2010/02/14)
A lyophilized pharmaceutical composition is described which contains Sodium [[3-(2-amino-1,2-dioxoethyl)-2-ethyl-1-phenylmethyl)-1H-indol-4-yl]oxy]acetate, a Solubilizer, and a Stabilizer. Such compositions are storage stable and readily dissolve in aqueous medium to give injectable solution for treatment of sepsis, etc.
Novel sPLA2 inhibitors
-
, (2008/06/13)
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.