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.
Regioselective synthesis of 4- and 7-alkoxyindoles from 2,3-dihalophenols: Application to the preparation of indole inhibitors of phospholipase A 2
Sanz, Roberto,Castroviejo, M. Pilar,Guilarte, Veronica,Perez, Antonio,Fananas, Francisco J.
, p. 5113 - 5118 (2008/02/05)
(Chemical Equation Presented) An efficient and regioselective synthesis of 4- and 7-alkoxyindoles has been developed from commercially available starting materials such as 3-halophenols and 3-chloroanisole. Directed ortho-metalation followed by two pallad
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.
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
-
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.
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.
Combination therapy for the treatment of inflammatory and respiratory diseases
-
, (2008/06/13)
A pharmaceutical composition for the treatment of Inflammatory Disease or Respiratory Disease in mammals, which comprises, as active ingredients, a neutrophil elastase inhibitor and an sPLA2 inhibitor.
Process for preparing toluenesulfinates
-
, (2008/06/13)
A process for preparing novel compounds useful in the preparation of 1H-indole-3-glyoxamides.
Method for the treatment of renal dysfunction with spla2 inhibitors
-
, (2008/06/13)
A method is disclosed for the treatment of of the symptoms associated with renal dysfunction by administering to an animal in need thereof a therapeutically effective amount of a sPLA2 inhibitor, such as a 1H-indole-3-glyoxylamide.
METHOD FOR TRATMENT OF NON-RHEUMATOID ARTHRITIS
-
, (2008/06/13)
A method is disclosed for the treatment of non-rheumatoid arthritis by administering to a mammal in need thereof a therapeutically effective amount of an sPLA 2 inhibitor.
