97077-43-5Relevant academic research and scientific papers
Indole-5-phenylcarbamate derivatives as human non-pancreatic secretory phospholipase A2 inhibitor
Liu, Ying,Han, Xiao-Feng,Huang, Chang-Kang,Hao, Xin,Lai, Lu-Hua
, p. 4540 - 4542 (2007/10/03)
The synthesis of the human non-pancreatic secretory phospholipase A2 inhibitor (IC50 = 1.81 ± 0.59 μM) is reported.
Synthesis of indomethacin analogues for evaluation as modulators of MRP activity
Maguire, Anita R.,Plunkett, Stephen J.,Papot, Sébastien,Clynes, Martin,O'Connor, Robert,Touhey, Samantha
, p. 745 - 762 (2007/10/03)
Synthesis of a range of indomethacin analogues, required for investigation in combination toxicity assays, bearing both N-benzyl and N-benzoyl groups, is described. Copyright
1H-INDOLE-3-ACETAMIDE SPLA2 INHIBITORS
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, (2008/06/13)
A class of novel 1-indole-3-acetamides represented by the formula; is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids.
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 1. Indole-3-acetamides
Dillard, Robert D.,Bach, Nicholas J.,Draheim, Susan E.,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. 5119 - 5136 (2007/10/03)
Phospholipases (PLAs) produce rate-limiting precursors in the biosynthesis of various types of biologically active lipids involved in inflammatory processes. Increased levels of human nonpancreatic secretory phospholipase A2 (hnps-PLA2) have been detected in several pathological conditions. An inhibitor of this enzyme could have therapeutic utility. A broad screening program was carried out to identify chemical structures which could inhibit hnps-PLA2. One of the lead compounds generated by the screening program was 5-methoxy-2-methyl-1-(phenylmethyl)-1H-indole-3-acetic acid (13a). We describe the syntheses, structure-activity relationships, and pharmacological activities of a series of indole-3-acetamides and related compounds derived from this lead. This SAR was undertaken with the aid of X- ray crystal structures of complexes between the inhibitors and hnps-PLA2 which were of great value in directing the SAR.
