Synthesis and carbonic anhydrase inhibitory properties of 1,3-dicarbonyl derivatives of methylaminobenzene-sulfonamide
Journal of Enzyme Inhibition and Medicinal Chemistry, vol.29, no.1, pp.132-136, 2014 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 29 Issue: 1
- Publication Date: 2014
- Doi Number: 10.3109/14756366.2012.757603
- Journal Name: Journal of Enzyme Inhibition and Medicinal Chemistry
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.132-136
- Keywords: 1,3-dicarbonyl, Carbonic anhydrase, Enzyme inhibitor, Sulfonamide
- Isparta University of Applied Sciences Affiliated: No
Abstract
1,3-Dicarbonyl derivatives of methylaminobenzene-sulfonamide were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and hCA II were evaluated. hCA I and hCA II from human erythrocytes were purified by a simple one-step procedure by using Sepharose 4B-L-tyrosine-sulfanilamide affinity column. Our results show that the synthesized compounds inhibited the activity of carbonic anhydrase (CA) I and CA II. Among them, 2b and 2e were found to be the most active (IC50 = 2.12 and 2.52 μM) for hCA I and hCA II, respectively. © 2014 Informa UK Ltd.