Synthesis of sulfonamide-containing N-hydroxyindole-2-carboxylates as inhibitors of human lactate dehydrogenase-isoform 5
2011
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
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 5.6μM) and behaved as competitive inhibitors versus both the substrate and the cofactor.
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