Twenty-four novel sulfonamide derivatives incorporating dipeptide tails were synthesized by facile acylation reactions of homosulfanilamide through benzotriazole or dicyclohexyl carbodiimide (DCC) mediated coupling reactions. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA IX and hCA XII. Most of the synthesized compounds showed good in vitro carbonic anhydrase inhibitory properties, with inhibition constants in the low nanomolar range. Particularly, the new dipeptide-sulfonamide conjugates incorporating Ala, Phe and Met in the dipeptide sequence, showed the most effective inhibitory activity against to CA IX and XII.

通过高硫磺酰胺通过苯并三唑或二环己基碳二亚胺（DCC）介导的偶联反应的轻松酰化反应，合成了包含二肽尾巴的二十四种新型磺酰胺衍生物。评估了新化合物的碳酸酐酶（CA，EC 4.2.1.1）对四种人（h）异构体hCA I，hCA II，hCA IX和hCA XII的抑制活性。大多数合成的化合物显示出良好的体外碳酸酐酶抑制特性，其抑制常数在低纳摩尔范围内。特别地，在二肽序列中结合了Ala，Phe和Met的新的二肽-磺酰胺缀合物显示出对CA IX和XII的最有效的抑制活性。