Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties
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 bicarbona...
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| Main Authors: | , , , , , , , , , , , |
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| Format: | Book |
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Taylor & Francis Group,
2017-01-01T00:00:00Z.
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|---|---|---|---|
| 001 | doaj_65d0bb06e87245b9a5a401ba32f4e19d | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Daniela De Vita |e author |
| 700 | 1 | 0 | |a Andrea Angeli |e author |
| 700 | 1 | 0 | |a Fabiana Pandolfi |e author |
| 700 | 1 | 0 | |a Martina Bortolami |e author |
| 700 | 1 | 0 | |a Roberta Costi |e author |
| 700 | 1 | 0 | |a Roberto Di Santo |e author |
| 700 | 1 | 0 | |a Elisabetta Suffredini |e author |
| 700 | 1 | 0 | |a Mariangela Ceruso |e author |
| 700 | 1 | 0 | |a Sonia Del Prete |e author |
| 700 | 1 | 0 | |a Clemente Capasso |e author |
| 700 | 1 | 0 | |a Luigi Scipione |e author |
| 700 | 1 | 0 | |a Claudiu T. Supuran |e author |
| 245 | 0 | 0 | |a Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties |
| 260 | |b Taylor & Francis Group, |c 2017-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2017.1327522 | ||
| 520 | |a 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. | ||
| 546 | |a EN | ||
| 690 | |a Carbonic anhydrase | ||
| 690 | |a sulfonamide | ||
| 690 | |a inhibitor | ||
| 690 | |a Vibrio cholerae | ||
| 690 | |a antibacterials | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 798-804 (2017) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2017.1327522 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/65d0bb06e87245b9a5a401ba32f4e19d |z Connect to this object online. |