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J Enzyme Inhib Med Chem. 2014 Feb;29(1):118-23. doi: 10.3109/14756366.2012.757222. Epub 2013 Jan 23.

In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II.

Author information

1
Department of Food Technology, Pamukova Vocational High School, Sakarya University , Sakarya , Turkey .

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.

PMID:
23339426
DOI:
10.3109/14756366.2012.757222
[Indexed for MEDLINE]

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