Spirobisnaphthalenes effectively inhibit carbonic anhydrase
| Autor: | Claudiu T. Supuran, Abdulselam Aslan, Hülya Göçer, İlhami Gülçin |
|---|---|
| Přispěvatelé: | Belirlenecek, GULCIN, Ilhami -- 0000-0001-5993-1668 |
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
Pharmacology
Gene isoform Carbonic anhydrase biology Dose-Response Relationship Drug Molecular Structure Chemistry Stereochemistry spirobisnaphthalenes General Medicine enzyme purification Naphthalenes Isozyme Isoenzymes Enzyme inhibition Structure-Activity Relationship Biochemistry Drug Discovery biology.protein Humans Spiro Compounds Carbonic Anhydrase Inhibitors enzyme inhibition Carbonic Anhydrases |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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