507271-76-3

Upstream product

• 3446-89-7 4-(Methylthio)benzaldehyde 
• 79-37-8 oxalyl dichloride 
• 507272-17-5 3-(2,4-difluorophenylsulfanyl)-6-methanesulfonyl-1H-indole-2-carboxylic acid methyl ester 
• 507272-16-4 2-carboxymethyl-6-methylsulfonylindole 
• 202584-19-8 methyl-2-azido-3-(4-methylthio-phenyl)propenoate 
• 202584-20-1 methyl-6-methylsulfanyl-1H-indole-2-carboxylate 
• 1996-44-7 2,4-difluorothiophenol 

Relevant academic research and scientific papers

Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors

The introduction of 3-arylmethyl, 3-aryloxy and 3-arylthio moieties into a 6-methylsulfonylindole framework using rational drug design led to potent, selective COX-2 inhibitors having efficacy in a rat carrageenan air pouch model. Incorporation of a conformationally more rigid 3-aroyloxy substituent onto the 6-methylsulfonylindole scaffold led to selective, but considerably less potent COX-2 inhibitors. Variation of the hydrophilicity and size of the indole 2-substituent of 3-arylthio-6-methylsulfonylindole inhibitors led to modulation of the COX-2 human whole blood (HWB) potency and selectivity. The introduction of 3-arylmethyl, 3-aryloxy and 3-arylthio moieties into a 6-methylsulfonylindole framework using rational drug design led to potent, selective COX-2 inhibitors having efficacy in a rat carrageenan air pouch model. Incorporation of a conformationally more rigid 3-aroyloxy substituent onto the 6- methylsulfonylindole scaffold led to selective, but considerably less potent COX-2 inhibitors. Variation of the hydrophilicity and size of the indole 2-substituent of 3-arylthio-6-methylsulfonylindole inhibitors led to modulation of the COX-2 human whole blood (HWB) potency and selectivity.

Indole derivatives as anti-inflammatory agents

This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents