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Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties.
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2017 Dec; Vol. 32 (1), pp. 798-804. - Publication Year :
- 2017
-
Abstract
- We discovered novel and selective sulfonamides/amides acting as inhibitors of the α-carbonic anhydrase (CA, EC 4.2.1.1) from the pathogenic bacterium Vibrio cholerae (VchCA). This Gram-negative bacterium is the causative agent of cholera and colonises the upper small intestine where sodium bicarbonate is present at a high concentration. The secondary sulfonamides and amides investigated here were potent, low nanomolar VchCA inhibitors whereas their inhibition of the human cytosolic isoforms CA I and II was in the micromolar range or higher. The molecules represent an interesting lead for antibacterial agents with a possibly new mechanism of action, although their CA inhibition mechanism is unknown for the moment.
- Subjects :
- Amides chemistry
Amides pharmacology
Carbonic Anhydrase I metabolism
Carbonic Anhydrase II metabolism
Carbonic Anhydrase Inhibitors chemical synthesis
Carbonic Anhydrase Inhibitors chemistry
Dose-Response Relationship, Drug
Humans
Imidazoles chemistry
Imidazoles pharmacology
Molecular Structure
Structure-Activity Relationship
Sulfonamides chemistry
Sulfonamides pharmacology
Carbonic Anhydrase I antagonists & inhibitors
Carbonic Anhydrase II antagonists & inhibitors
Carbonic Anhydrase Inhibitors pharmacology
Vibrio cholerae enzymology
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 32
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 28569564
- Full Text :
- https://doi.org/10.1080/14756366.2017.1327522