85753-64-6

Upstream product

• 109-83-1 (2-hydroxyethyl)(methyl)amine 
• 98-09-9 benzenesulfonyl chloride 

Downstream Products

• 1416133-67-9 1-[2-(N-methylphenylsulfonamido)ethyl]-1H-1,2,3-triazole-4,5-dicarboxylic acid 
• 1416133-78-2 C₉H₁₂N₄O₂S 
• 86227-37-4 N-benzenesulfonyl 4-(3',4'-dimethoxyphenyl)-4-methylaminoethylcyclohex-2-en-1-one 
• 86227-38-5 N-{2-[1-(3,4-Dimethoxy-phenyl)-4-hydroxy-cyclohex-2-enyl]-ethyl}-N-methyl-benzenesulfonamide 
• 85753-67-9 N-[3-(3,4-Dimethoxy-phenyl)-3-[1,3]dioxolan-2-yl-propyl]-N-methyl-benzenesulfonamide 
• 86227-35-2 N-[3-(3,4-Dimethoxy-phenyl)-4-oxo-butyl]-N-methyl-benzenesulfonamide 
• 85753-65-7 N-[3-Cyano-3-(3,4-dimethoxy-phenyl)-propyl]-N-methyl-benzenesulfonamide 

Relevant academic research and scientific papers

SCELETIUM (AIZOACEAE) ALKALOIDS: TOTAL SYNTHESIS OF RACEMIC MESEMBRANONE, JOUBERTINAMINE AND EPIJOUBERTINAMINE

The total synthesis of the Sceletium alkaloids mesembranone, joubertinamine and epijoubertinamine via the intramolecular cyclization of an enone to a benzensulfonamide grouping under the conditions of a dissolving metal reduction is described.

Fragment-based discovery of novel and selective mPGES-1 inhibitors Part 1: Identification of sulfonamido-1,2,3-triazole-4,5-dicarboxylic acid

Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible prostaglandin E synthase that catalyzes the conversion of prostaglandin PGH 2 to PGE2 and represents a novel target for therapeutic treatment of inflammatory disorders. It is essential to identify mPGES-1 inhibitor with novel scaffold as new hit or lead compound for the purpose of the next-generation anti-inflammatory drugs. Herein we report the discovery of sulfonamido-1,2,3-triazole-4,5-dicarboxylic derivatives as a novel class of mPGES-1 inhibitors identified through fragment-based virtual screening and in vitro assays on the inhibitory activity of the actual compounds. 1-[2-(N-Phenylbenzenesulfonamido)ethyl]-1H-1,2,3-triazole-4,5-dicarboxylic acid (6f) inhibits human mPGES-1 (IC50 of 1.1 μM) with high selectivity (ca.1000-fold) over both COX-1 and COX-2 in a cell-free assay. In addition, the activity of compound 6f was again tested at 10 μM concentration in presence of 0.1% Triton X-100 and found to be reduced to 1/4 of its original activity without this detergent. Compared to the complete loss of activity of nuisance inhibitor with the detergent, therefore, compound 6f would be regarded as a partial nuisance inhibitor of mPGES-1 with a novel scaffold for the optimal design of more potent mPGES-1 inhibitors.