title: In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II.
abstract: In this study, in vitro 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-(p-tolylthiourenyl) saccharin (6m) was found to be the most active one for hCA I activity (IC50=13.67 μM) and 6-(m-methoxyphenylurenyl) saccharin (6b) 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 (6l--v) inhibited more hCA I and hCA II than urea derivatives (6a-k). All compounds (excluding 6c and 6r) have higher inhibitory activity on hCA II than on hCA I.
authors: Department of Food Technology, Pamukova Vocational High School, Sakarya University , Sakarya , Turkey .
authors: Fatih
authors: F
authors: Sonmez
authors: Cigdem
authors: C
authors: Bilen
authors: Sinem
authors: S
authors: Sumersan
authors: Nahit
authors: N
authors: Gencer
authors: Semra
authors: S
authors: Isik
authors: Oktay
authors: O
authors: Arslan
authors: Mustafa
authors: M
authors: Kucukislamoglu
mesh_terms: D024401:Carbonic Anhydrase I / Q000378:metabolism*; D024402:Carbonic Anhydrase II / Q000378:metabolism*; D004912:Erythrocytes / Q000201:enzymology*; D066298:In Vitro Techniques; D012439:Saccharin / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II; D012439:Saccharin