A series of selenides bearing benzensulfonamide were investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Potent inhibitory action, in the low nanomolar range, was detected against isoforms hCA II and VII, which are known to be involved in neuropathic pain modulation. These selenides showed on the other hand moderate inhibition against the cytosolic isoforms hCA I and transmembrane hCA IX. X-ray crystallographic data of two derivatives bound to hCA II allowed us to rationalize the excellent inhibitory data. In a mice model of neuropathic pain induced by oxaliplatin, some of the strong CA II/VII inhibitors induced a long lasting pain relieving effect.

研究了一系列带有苯甲磺酰胺的硒化物作为金属酶碳酸酐酶的抑制剂（CA，EC 4.2.1.1）。已检测到针对同工型hCA II和VII的低纳摩尔浓度范围的有效抑制作用，这些同型异构体已知参与神经性疼痛调节。另一方面，这些硒化物显示出对胞质同工型hCA I和跨膜hCA IX的中等抑制作用。与hCA II结合的两种衍生物的X射线晶体学数据使我们合理化了优异的抑制数据。在由奥沙利铂诱导的神经性疼痛的小鼠模型中，一些强效的CA II / VII抑制剂可诱导持久的缓解疼痛的作用。