Abdoli Morteza, Bozdag Murat, Angeli Andrea, Supuran Claudiu T
Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Via U. Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Department of Chemistry, Faculty of Science, Lorestan University, Khorramabad 6813833946, Iran.
Metabolites. 2018 Jun 1;8(2):37. doi: 10.3390/metabo8020037.
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 (Ks of 5.3⁻334 nM). The β- and γ-class CAs from pathogenic bacteria and fungi, such as and , 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.
通过使4-氨磺酰基苯甲酸与伯胺、仲胺和氨基酸反应，得到了一系列含有4-氨磺酰基部分的苯甲酰胺。这些磺酰胺被作为金属酶碳酸酐酶（CA，EC 4.2.1.1）的抑制剂进行研究。人（h）同工型hCA II、VII和IX在低纳摩尔或亚纳摩尔范围内受到抑制，而hCA I对抑制的敏感性稍低（Ks为5.3⁻334 nM）。本文报道的磺酰胺在微摩尔范围内抑制来自致病细菌和真菌的β-和γ-类碳酸酐酶，如 和 。苯甲酰胺-4-磺酰胺是一类很有前景的高效碳酸酐酶抑制剂。
