1. Spirobisnaphthalenes effectively inhibit carbonic anhydrase.
- Author
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Gocer H, Aslan A, Gülçin İ, and Supuran CT
- Subjects
- Carbonic Anhydrase Inhibitors chemical synthesis, Carbonic Anhydrase Inhibitors chemistry, Dose-Response Relationship, Drug, Humans, Isoenzymes antagonists & inhibitors, Isoenzymes metabolism, Molecular Structure, Naphthalenes chemical synthesis, Naphthalenes chemistry, Spiro Compounds chemical synthesis, Spiro Compounds chemistry, Structure-Activity Relationship, Carbonic Anhydrase Inhibitors pharmacology, Carbonic Anhydrases metabolism, Naphthalenes pharmacology, Spiro Compounds pharmacology
- Abstract
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 Ki values were similar for both CA isoenzymes, the compounds showing good inhibitory activity. Ki values ranged between 1.60 and 460.42 µM for hCA I and between 0.39 and 419.42 µM 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.
- Published
- 2016
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