172732-89-7Relevant academic research and scientific papers
Method for treating sepsis
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, (2008/06/13)
A novel method of treating and/or preventing sepsis.
Morpholino-N-ethyl ester prodrugs of indole sPLA2 inhibitors
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, (2008/06/13)
The compound, ((3(2-amino-1,2-dioxoethyl)-1-((1,1′-biphenyl)-3-ylmethyl)-2-methyl-1H-indol-4-yl)oxy)acetic acid morpholino-ethyl ester, is disclosed together with its use as a highly bioavailable indole compound for inhibiting sPLA2mediated release of fatty acids for treatment of conditions such as septic shock.
Method for treatment of chronic bronchitis using indole compounds
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, (2008/06/13)
A method is disclosed for the treatment of chronic bronchitis by administering to a mammal in need thereof a therapeutically effective amount of a 1H-indole-3-glyoxylamide compound.
1H-INDOLE-3-GLYOXYLAMIDE SPLA2 INHIBITORS
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, (2008/06/13)
A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty adds for treatment of conditions such as septic shock
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides
Draheim, Susan E.,Bach, Nicholas J.,Dillard, Robert D.,Berry, Dennis R.,Carlson, Donald G.,Chirgadze, Nickolay Y.,Clawson, David K.,Hartley, Lawrence W.,Johnson, Lea M.,Jones, Noel D.,McKinney, Emma R.,Mihelich, Edward D.,Olkowski, Jennifer L.,Schevitz, Richard W.,Smith, Amy C.,Snyder, David W.,Sommers, Cynthia D.,Wery, Jean-Pierre
, p. 5159 - 5175 (2007/10/03)
The preceding papers of this series detail the development of functionalized indole-3-acetamides as inhibitors of hnps-PLA2. We describe here the extension of the structure-activity relationship to include a series of indole-3-glyoxamide derivatives. Functionalized indole-3-glyoxamides with an acidic substituent appended to the 4- or 5-position of the indole ring were prepared and tested as inhibitors of hnps-PLA2. It was found that the indole-3-glyoxamides with a 4-oxyacetic acid substituent had optimal inhibitory activity. These inhibitors exhibited an improvement in potency over the best of the indole-3-acetamides, and LY315920 (6m) was selected for evaluation clinically as an hnps-PLA2 inhibitor.
