Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 28, Issue 2, Pages 407-411Publisher
INFORMA HEALTHCARE
DOI: 10.3109/14756366.2011.641015
Keywords
Carbonic anhydrase; dithiocarbamate; beta-class enzyme; inhibitor; Mycobacterium tuberculosis
Funding
- EU FP7 research grant (Metoxia project)
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A series of N-mono- and N,N-disubstituted dithiocarbamates have been investigated as inhibitors of two beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogen Mycobacterium tuberculosis, mtCA 1 (Rv1284) and mtCA 3 (Rv3273). Both enzymes were inhibited with efficacies between the subnanomolar to the micromolar one, depending on the substitution pattern at the nitrogen atom from the dithiocarbamate zinc-binding group. Aryl, arylalkyl-, heterocyclic as well as aliphatic and amino acyl such moieties led to potent mtCA 1 and 3 inhibitors in both the N-mono- and N,N-disubstituted dithiocarbamate series. This new class of beta-CA inhibitors may have the potential for developing antimycobacterial agents with a diverse mechanism of action compared to the clinically used drugs for which many strains exhibit multi-drug/extensive multi-drug resistance.
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