Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370143 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
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 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.
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Organic Chemistry
Authors
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,