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Metabolites 2018, 8(2), 37; https://doi.org/10.3390/metabo8020037

Benzamide-4-Sulfonamides Are Effective Human Carbonic Anhydrase I, II, VII, and IX Inhibitors

1
Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Via U. Schiff 6, Sesto Fiorentino, 50019 Florence, Italy
2
Department of Chemistry, Faculty of Science, Lorestan University, Khorramabad 6813833946, Iran
*
Authors to whom correspondence should be addressed.
Received: 11 May 2018 / Revised: 26 May 2018 / Accepted: 30 May 2018 / Published: 1 June 2018
(This article belongs to the Special Issue Carbonic Anhydrases and Metabolism)
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Abstract

A series of benzamides incorporating 4-sulfamoyl moieties were obtained by reacting 4-sulfamoyl benzoic acid with primary and secondary amines and amino acids. These sulfonamides were investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). The human (h) isoforms hCA II, VII, and IX were inhibited in the low nanomolar or subnanomolar ranges, whereas hCA I was slightly less sensitive to inhibition (KIs of 5.3–334 nM). The β- and γ-class CAs from pathogenic bacteria and fungi, such as Vibrio cholerae and Malassezia globosa, were inhibited in the micromolar range by the sulfonamides reported in the paper. The benzamide-4-sulfonamides are a promising class of highly effective CA inhibitors. View Full-Text
Keywords: carbonic anhydrase; human isoform; sulfonamide; benzamide; pathogens carbonic anhydrase; human isoform; sulfonamide; benzamide; pathogens
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Abdoli, M.; Bozdag, M.; Angeli, A.; Supuran, C.T. Benzamide-4-Sulfonamides Are Effective Human Carbonic Anhydrase I, II, VII, and IX Inhibitors. Metabolites 2018, 8, 37.

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