1303574-30-2Relevant academic research and scientific papers
Synthesis of sulfonamide-containing N-hydroxyindole-2-carboxylates as inhibitors of human lactate dehydrogenase-isoform 5
Granchi, Carlotta,Roy, Sarabindu,Mottinelli, Marco,Nardini, Elisa,Campinoti, Fabio,Tuccinardi, Tiziano,Lanza, Mario,Betti, Laura,Giannaccini, Gino,Lucacchini, Antonio,Martinelli, Adriano,MacChia, Marco,Minutolo, Filippo
supporting information; experimental part, p. 7331 - 7336 (2012/02/04)
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.
