Carlotta Granchi,
Sarabindu Roy, Marco Mottinelli,
Elisa Nardini,
Fabio Campinoti,
Tiziano Tuccinardi,
Mario Lanza,
Laura Betti,
Gino Giannaccini,
Antonio Lucacchini,
Adriano Martinelli,
Marco Macchia,
Filippo Minutolo
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ABSTRACT: 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 K(i) 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 (K(i) values as low as 5.6 μM) and behaved as competitive inhibitors versus both the substrate and the cofactor.
Bioorganic & medicinal chemistry letters 10/2011; 21(24):7331-6. · 2.65 Impact Factor
