关于肼基苯磺酰胺类化合物作为人碳酸酐酶 I、II、IX 和 XII 抑制剂的研究。
Investigation on Hydrazonobenzenesulfonamides as Human Carbonic Anhydrase I, II, IX and XII Inhibitors.
机构信息
Department of Life and Environmental Sciences, University of Cagliari, University Campus, S.P. 8 CA, 09042 Monserrato, Italy.
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano,Via Mangiagalli 25, 20133 Milano, Italy.
出版信息
Molecules. 2022 Dec 22;28(1):91. doi: 10.3390/molecules28010091.
A small series of hydrazonobenzenesulfonamides was designed, synthesized and studied for their human carbonic anhydrase (hCA) inhibitory activity. The synthesized compounds were evaluated against hCA I, II, IX and XII isoforms using acetazolamide (AAZ) as the standard inhibitor. Various hydrazonosulfonamide derivatives showed inhibitory activity at low nanomolar levels with selectivity against the cytosolic hCA II isoform, as well as the transmembrane, tumor-associated enzymes hCA IX and XII. The most potent and selective hydrazones , , , , and were docked into isoforms I, II, IX and XII to better understand their activity and selectivity for the different CA isoforms.
设计、合成了一系列腙苯磺酰胺类化合物，并研究了它们对人碳酸酐酶（hCA）的抑制活性。以乙酰唑胺（AAZ）为标准抑制剂，对合成的化合物进行了人碳酸酐酶 I、II、IX 和 XII 同工酶的活性评价。各种腙磺酰胺衍生物以低纳摩尔水平表现出抑制活性，对细胞质 hCA II 同工酶以及跨膜、肿瘤相关酶 hCA IX 和 XII 具有选择性。最有效和最具选择性的腙类化合物 、 、 、 、 和 被对接到人碳酸酐酶 I、II、IX 和 XII 同工酶中，以更好地理解它们对不同 CA 同工酶的活性和选择性。
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