期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 28, 期 2, 页码 384-387出版社
INFORMA HEALTHCARE
DOI: 10.3109/14756366.2011.645539
关键词
Carbonic anhydrase; beta-carbonic anhydrase; sulfonamide; dihalogenated sulfanilamide/benzolamide; enzyme inhibitor; Mycobacterium tuberculosis
资金
- EU
A series of halogenated sulfanilamides and halogenated benzolamide derivatives have been investigated as inhibitors of three beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogen Mycobacterium tuberculosis, mtCA 1 (Rv1284), mtCA 2 (Rv3588c) and mtCA 3 (Rv3273). All three enzymes were inhibited with efficacies between the submicromolar to the micromolar one, depending on the substitution pattern at the sulfanilamide moiety/fragment of the molecule. Best inhibitors were the halogenated benzolamides (K(I)s in the range of 0.12-0.45 mu M) whereas the halogenated sulfanilamides were slightly less inhibitory (K(I)s in the range of 0.41-4.74 mu M). This 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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