Herein we report on a new series of hydrazidoureidobenzensulfonamides investigated as inhibitors of the cytosolic human (h) hCA I and II isoforms, as well as the transmembrane, tumor-associated enzymes hCA IX and XII. The reported derivatives contain a 4-substituted piperidine fragment in which the hydrazidoureido linker has been involved as spacer between the benzenesulfonamide fragment which binds the zinc ion from the active site, and the tail of the inhibitor. Depending on the substitution pattern at the piperidine ring, low nanomolar inhibitors were detected against hCA II, hCA IX and hCA XII, making the new class of sulfonamides of interest for various pharmacologic applications.

中文翻译：

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哌啶基-肼基脲基连接基对苯磺酰胺化合物的应用：强力碳酸酐酶II，IX和XII抑制剂的合成，体外和计算机评估。

在本文中，我们报道了一系列新的肼基脲基苯甲磺酰胺类药物，它们被研究为胞质人（h）hCA I和II同种型以及跨膜的肿瘤相关酶hCA IX和XII的抑制剂。报道的衍生物含有4-取代的哌啶片段，其中酰脲脲基接头作为间隔物，该间隔物结合了来自活性位点的锌离子的苯磺酰胺片段和抑制剂的尾部。根据哌啶环上的取代模式，检测到针对hCA II，hCA IX和hCA XII的低纳摩尔抑制剂，这使得新的一类磺酰胺类药物可用于各种药理应用。