Source:http://linkedlifedata.com/resource/pubmed/id/20006931
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
A novel proton transfer compound, pyridin-2-ylmethanaminium 2,4-dichloro-5-sulfamoylbenzoate (1), and a mixed-ligand Zn(II) complex, bis(2,4-dichloro-5-sulfamoylbenzoate)(2-aminomethylpyridine)aquazinc(II) monohydrate (2), have been synthesized from the same free ligands, which are 2,4-dichloro-5-sulfamoylbenzoic acid (Hsba) and 2-aminomethylpyridine (amp). They have been characterized by elemental, spectral ((1)H NMR, IR and UV-vis.) and thermal analyses. Additionally, magnetic measurement and single crystal X-ray diffraction technique were applied to compound 2. In the complex, Zn(II) ion exhibits a distorted octahedral configuration coordinated by O1 and O1(i) atoms of two mono dentante sba anions and N1, N2, N2(i) atoms of bidentante amp anion and a water molecule (O1w). The free ligands Hsba and amp, and the products 1 and 2, and acetazolamide (AAZ) as the control compound, were also evaluated for their in vitro inhibitor effects on human Carbonic Anhydrase isoenzymes (hCA I and hCA II) purified from erythrocyte cell by affinity chromatography for their hydratase and esterase activities. The IC(50) values of products 1 and 2 for hydratase activity are 0.26 and 0.13microM for hCA I and 0.30 and 0.15microM for hCA II, respectively. The IC(50) values of the same inhibitors for esterase activity are 0.32 and 0.045microM for hCA I and 0.29 and 0.23microM for hCA II, respectively. In relation to esterase activities, the inhibition equilibrium constants (K(i)) were also determined and found 0.25 and 0.058microM on hCA I and 0.22 and 0.24microM on hCA II for 1 and 2, respectively. The comparison of the inhibition studies of newly synthesized compounds 1 and 2 to parent compounds Hsba and amp and to AAZ indicated that 1 and 2 have effective inhibitory activity on hCA I and II, and might be used potential inhibitors.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrase I,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrase II,
http://linkedlifedata.com/resource/pubmed/chemical/Carbonic Anhydrase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Organometallic Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Protons,
http://linkedlifedata.com/resource/pubmed/chemical/Zinc
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
930-8
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pubmed:meshHeading |
pubmed-meshheading:20006931-Carbonic Anhydrase I,
pubmed-meshheading:20006931-Carbonic Anhydrase II,
pubmed-meshheading:20006931-Carbonic Anhydrase Inhibitors,
pubmed-meshheading:20006931-Crystallography, X-Ray,
pubmed-meshheading:20006931-Erythrocytes,
pubmed-meshheading:20006931-Glaucoma,
pubmed-meshheading:20006931-Humans,
pubmed-meshheading:20006931-Ligands,
pubmed-meshheading:20006931-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20006931-Models, Molecular,
pubmed-meshheading:20006931-Organometallic Compounds,
pubmed-meshheading:20006931-Protons,
pubmed-meshheading:20006931-Spectroscopy, Fourier Transform Infrared,
pubmed-meshheading:20006931-Structure-Activity Relationship,
pubmed-meshheading:20006931-Temperature,
pubmed-meshheading:20006931-Zinc
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex.
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pubmed:affiliation |
Department of Chemistry, Faculty of Arts and Sciences, Dumlupinar University, 43100 Kütahya, Turkey. yenikaya@dumlupinar.edu.tr
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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