In vitro inhibition effect and structure–activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II. (February 2014)

• Record Type: Journal Article
• Authors: Sonmez, Fatih; Bilen, Cigdem; Sumersan, Sinem; Gencer, Nahit; Isik, Semra; Arslan, Oktay; Kucukislamoglu, Mustafa
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 29:Number 1(2014:Feb.)
• Page Start: 118
• Page End: 123
• Publication Date: 2014-02
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2012.757222
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title>Abstract</title> <p>In this study, <italic>in vitro</italic> inhibitory effects of some saccharin derivatives on purified carbonic anhydrase I and II were investigated using CO₂ as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among the compounds, 6-(<italic>p</italic>-tolylthiourenyl) saccharin (<bold>6m</bold>) was found to be the most active one for hCA I activity (IC₅₀ = 13.67 μM) and 6-(<italic>m</italic>-methoxyphenylurenyl) saccharin (<bold>6b</bold>) was found to be the most active one for hCA II activity (IC₅₀ = 6.54 μM). Structure–activity relationships (SARs) study showed that, generally, thiourea derivatives (<bold>6l--v</bold>) inhibited more hCA I and hCA II than urea derivatives (<bold>6a–k</bold>). All compounds (excluding <bold>6c</bold> and <bold>6r)</bold> have higher inhibitory activity on hCA II than on hCA I.</p> </abstract>