1069042-93-8

Upstream product

• 104-92-7 1-bromo-4-methoxy-benzene 
• 1069047-06-8 methyl 3-[3-(2-phenylethyl)-1H-indol-5-yl]propanoate 
• 127876-36-2 2-(benzotriazol-1-yl)acetophenone 
• 1069051-39-3 1-(5-bromo-1H-indol-3-yl)-2-phenylethanone 
• 1069051-42-8 5-bromo-3-(2-phenylethyl)-1H-indole 
• 1069047-04-6 methyl (2E)-3-[3-(2-phenylethyl)-1H-indol-5-yl]-2-propenoate 

Downstream Products

• 1069042-95-0 3-[1-(4-methoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid 
• 1069047-11-5 3-[1-(4-methoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid tromethamine salt 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of 3-(1-aryl-1 h -indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase a2α inhibitors

This article describes the design, synthesis, and biological evaluation of new indole-based cytosolic phospholipase A2α (cPLA2α, a group IVA phospholipase A2) inhibitors. A screening-hit compound from our library, (E)-3-{4-[(4-chlorophenyl)thio]-3-nitrophenyl}acrylic acid (5), was used to design a class of 3-(1-aryl-1H-indol-5-yl)propanoic acids as new small molecule inhibitors. The resultant structure-activity relationships studied using the isolated enzyme and by cell-based assays revealed that the 1-(p-O-substituted)phenyl, 3-phenylethyl, and 5-propanoic acid groups on the indole core are essential for good inhibitory activity against cPLA2α. Optimization of the p-substituents on the N1 phenyl group led to the discovery of 56n (ASB14780), which was shown to be a potent inhibitor of cPLA2α via enzyme assay, cell-based assay, and guinea pig and human whole-blood assays. It displayed oral efficacy toward mice tetradecanoyl phorbol acetate-induced ear edema and guinea pig ovalbumin-induced asthma models.

INDOLE DERIVATIVE HAVING CPLA2 INHIBITORY ACTIVITY, USE OF THE SAME AND METHOD FOR PRODUCING THE SAME

A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.