1303571-68-7

Upstream product

• 616-83-1 4-methyl-3-nitrobenzenesulfonyl chloride 
• 932-96-7 N-methyl(p-chloroaniline) 
• 1303576-61-5 methyl 6-(N-(4-chlorophenyl)-N-methylsulfamoyl)-1-hydroxy-1H-indole-2-carboxylate 
• 1303573-31-0 N-(4-chlorophenyl)-N,4-dimethyl-3-nitrobenzenesulfonamide 
• 1303574-98-2 C₁₇H₁₅ClN₂O₇S 

Relevant academic research and scientific papers

COMPOUNDS INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH) AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS

The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.

Synthesis of sulfonamide-containing N-hydroxyindole-2-carboxylates as inhibitors of human lactate dehydrogenase-isoform 5

N-Hydroxyindole-2-carboxylates possessing sulfonamide-substituents at either position 5 or 6 were designed and synthesized. The inhibitory activities of these compounds against isoforms 1 and 5 of human lactate dehydrogenase were analysed, and Ki values of the most efficient inhibitors were determined by standard enzyme kinetic studies. Some of these compounds displayed state-of-the-art inhibitory potencies against isoform 5 (Ki values as low as 5.6 μM) and behaved as competitive inhibitors versus both the substrate and the cofactor.