Sulfamide was desymmetrized by a reaction with aldehydes to give -sulfamoylimines. The latter reagents were successfully introduced into diastereo- and chemoselective transformation with cyclic anhydride using the Castagnoli-Cushman reaction to give unprotected -sulfamoyl tetrahydroisoquinolonic (THIQ) acids under simple metal-free protocol. Thereby, the first general approach to the direct assembly of six-membered -sulfamoyl lactams was developed. The synthesized compounds belong to representative, drug-like chemotypes with their well-defined three-dimensional structures and tunable physicochemical properties. In an attempt to probe their pharmacological potential, the newly synthesized lactams were screened against therapeutically relevant human and bacterial carbonic anhydrases, with some derivatives showing low micromolar enzyme inhibitory profiles.

中文翻译：

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基于磺酰胺去对称化和 Castagnoli-Cushman 反应直接组装带有锌结合基团的 N-氨磺酰内酰胺支架用于抑制金属酶

磺酰胺通过与醛反应而去对称化，得到β-氨磺酰亚胺。使用 Castagnoli-Cushman 反应，将后一种试剂成功引入环酸酐的非对映和化学选择性转化中，在简单的无金属方案下得到未保护的氨磺酰四氢异喹啉 (THIQ) 酸。由此，开发了第一个直接组装六元氨磺酰内酰胺的通用方法。合成的化合物属于具有代表性的类药物化学型，具有明确的三维结构和可调节的理化性质。为了探索其药理学潜力，新合成的内酰胺针对治疗相关的人类和细菌碳酸酐酶进行了筛选，其中一些衍生物显示出低微摩尔酶抑制谱。