A series of 3H-1,2-benzoxathiepine 2,2-dioxides incorporating 7-acylamino moieties were obtained by an original procedure starting from 5-nitrosalicylaldehyde, which was treated with propenylsulfonyl chloride followed by Wittig reaction of the bis-olefin intermediate. The new derivatives, belonging to the homosulfocoumarin chemotype, were assayed as inhibitors of the zinc metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Four pharmacologically relevant human (h) isoforms were investigated, the cytosolic hCA I and II and the transmembrane, tumour-associated hCA IX and XII. No relevant inhibition of hCA I and II was observed, whereas some of the new derivatives were effective, low nanomolar hCA IX/XII inhibitors, making them of interest for investigations in situations in which the activity of these isoforms is overexpressed, such as hypoxic tumours, arthritis or cerebral ischaemia.

中文翻译：

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7-酰基氨基-3H-1,2-苯并x庚因2,2-二氧化物作为新型同工型选择性碳酸酐酶IX和XII抑制剂。

从5-硝基水杨醛开始，通过原始程序获得了一系列结合有7-酰基氨基部分的3H-1,2-苯并噻庚因2,2-二氧化物，将其用丙烯磺酰氯处理，然后使双烯烃中间体进行Wittig反应。测定属于高磺香豆素化学型的新衍生物作为锌金属酶碳酸酐酶的抑制剂（CA，EC 4.2.1.1）。研究了四种与药理相关的人类（h）亚型，即胞质hCA I和II以及跨膜，与肿瘤相关的hCA IX和XII。并未观察到对hCA I和II的相关抑制作用，而一些新的衍生物是有效的低纳摩尔hCA IX / XII抑制剂，这使它们成为研究这些亚型活性过高的情况的兴趣，