| In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II. | |
MedLine Citation:
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PMID: 23339426 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Abstract In this study, in vitro inhibitory effects of some saccharin derivatives on purified carbonic anhydrase I and II were investigated using CO(2) 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 (IC(50) = 13.67 μM) and 6-(m-methoxyphenylurenyl) saccharin (6b) was found to be the most active one for hCA II activity (IC(50) = 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:
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Fatih Sonmez; Cigdem Bilen; Sinem Sumersan; Nahit Gencer; Semra Isik; Oktay Arslan; Mustafa Kucukislamoglu |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2013-1-23 |
Journal Detail:
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Title: Journal of enzyme inhibition and medicinal chemistry Volume: - ISSN: 1475-6374 ISO Abbreviation: J Enzyme Inhib Med Chem Publication Date: 2013 Jan |
Date Detail:
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Created Date: 2013-1-23 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101150203 Medline TA: J Enzyme Inhib Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Department of Food Technology, Pamukova Vocational High School, Sakarya University , Sakarya , Turkey . |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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