Spirobisnaphthalenes effectively inhibit carbonic anhydrase

摘要

This study explores the correlation between human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II (hCA I, II) and the inhibitory features of some spirobisnaphthalene derivatives. A group of spirobisnaphthalenes was synthesized and their hCA I and II inhibitory effects was investigated. The K-i values were similar for both CA isoenzymes, the compounds showing good inhibitory activity. K-i values ranged between 1.60 and 460.42 mu M for hCA I and between 0.39 and 419.42 mu M for hCA II, respectively. The spirobisnaphthalenes derivatives might be useful for designing CA inhibitors belonging to novel chemotypes compared to the highly investigated sulfonamides, sulfamates or coumarins.