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  1. Article ; Online: Quinoline-sulfamoyl carbamates/sulfamide derivatives: Synthesis, cytotoxicity, carbonic anhydrase activity, and molecular modelling studies.

    Cakmak, Elmas Begum / Zengin Kurt, Belma / Ozturk Civelek, Dilek / Angeli, Andrea / Akdemir, Atilla / Sonmez, Fatih / Supuran, Claudiu T / Kucukislamoglu, Mustafa

    Bioorganic chemistry

    2021  Volume 110, Page(s) 104778

    Abstract: Carbonic anhydrase (CA) IX, and XII isoforms are known to be highly expressed in various human tissues and malignancies. CA IX is a prominent target for some cancers because it is overexpressed in hypoxic tumors and this overexpression leads to poor ... ...

    Abstract Carbonic anhydrase (CA) IX, and XII isoforms are known to be highly expressed in various human tissues and malignancies. CA IX is a prominent target for some cancers because it is overexpressed in hypoxic tumors and this overexpression leads to poor prognosis. Novel twenty-seven compounds in two series (sulfamoylcarbamate-based quinoline (2a-2o) and sulfamide-based quinoline (3a-3l)) were synthesized and characterized by means of IR, NMR, and mass spectra. Their inhibitory activities were evaluated against CA I, CA II, CA IX, and CA XII isoforms. 2-Phenylpropyl (N-(quinolin-8-yl)sulfamoyl)carbamate (2m) exhibited the highest hCA IX inhibition with the K
    MeSH term(s) Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Antioxidants/chemical synthesis ; Antioxidants/chemistry ; Antioxidants/pharmacology ; Carbamates/chemistry ; Carbamates/pharmacology ; Carbonic Anhydrase Inhibitors/chemical synthesis ; Carbonic Anhydrase Inhibitors/chemistry ; Carbonic Anhydrase Inhibitors/pharmacology ; Carbonic Anhydrases/metabolism ; Cell Line ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Models, Molecular ; Molecular Structure ; Quinolines/chemistry ; Quinolines/pharmacology ; Structure-Activity Relationship ; Sulfonamides/chemistry ; Sulfonamides/pharmacology ; Sulfonic Acids/chemistry ; Sulfonic Acids/pharmacology
    Chemical Substances Antineoplastic Agents ; Antioxidants ; Carbamates ; Carbonic Anhydrase Inhibitors ; Quinolines ; Sulfonamides ; Sulfonic Acids ; sulfamic acid (9NFU33906Q) ; quinoline (E66400VT9R) ; Carbonic Anhydrases (EC 4.2.1.1)
    Language English
    Publishing date 2021-02-24
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2021.104778
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    Zs.A 4207: Show issues Location:
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  2. Article ; Online: Synthesis, antioxidant activity and SAR study of novel spiro-isatin-based Schiff bases.

    Sonmez, Fatih / Gunesli, Zuhal / Kurt, Belma Zengin / Gazioglu, Isil / Avci, Davut / Kucukislamoglu, Mustafa

    Molecular diversity

    2019  Volume 23, Issue 4, Page(s) 829–844

    Abstract: A new series of 21 Schiff bases of spiro-isatin was synthesized, and their DPPH, CUPRAC and ABTS cation radical scavenging abilities were investigated for antioxidant activity. The results showed that all the synthesized compounds exhibited antioxidant ... ...

    Abstract A new series of 21 Schiff bases of spiro-isatin was synthesized, and their DPPH, CUPRAC and ABTS cation radical scavenging abilities were investigated for antioxidant activity. The results showed that all the synthesized compounds exhibited antioxidant activity for each assay. 5̍-(2,3-Dihydroxybenzylideneamino)spiro[[1,3] dioxolane-2,3̍-indoline]-2̍-on (5c) (IC
    MeSH term(s) Antioxidants/chemical synthesis ; Antioxidants/chemistry ; Benzothiazoles/chemistry ; Biphenyl Compounds/chemistry ; Copper/chemistry ; Isatin/chemical synthesis ; Isatin/chemistry ; Picrates/chemistry ; Schiff Bases/chemical synthesis ; Schiff Bases/chemistry ; Spiro Compounds/chemical synthesis ; Spiro Compounds/chemistry ; Structure-Activity Relationship ; Sulfonic Acids/chemistry
    Chemical Substances Antioxidants ; Benzothiazoles ; Biphenyl Compounds ; Picrates ; Schiff Bases ; Spiro Compounds ; Sulfonic Acids ; 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid (28752-68-3) ; Copper (789U1901C5) ; Isatin (82X95S7M06) ; 1,1-diphenyl-2-picrylhydrazyl (DFD3H4VGDH)
    Language English
    Publishing date 2019-01-05
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1376507-3
    ISSN 1573-501X ; 1381-1991
    ISSN (online) 1573-501X
    ISSN 1381-1991
    DOI 10.1007/s11030-018-09910-7
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 4946: Show issues Location:
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  3. Article ; Online: Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives.

    Kurt, Belma Zengin / Gazioglu, Isil / Sonmez, Fatih / Kucukislamoglu, Mustafa

    Bioorganic chemistry

    2015  Volume 59, Page(s) 80–90

    Abstract: A newly series of coumarylthiazole derivatives containing aryl urea/thiourea groups were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized ... ...

    Abstract A newly series of coumarylthiazole derivatives containing aryl urea/thiourea groups were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized compounds exhibited inhibitory activity to both cholinesterases. Among them, 1-(4-(8-methoxy-2-oxo-2H-chromen-3-yl)thiazol-2-yl)-3-(4-chlorophenyl)thiourea (f8, IC50 = 4.58 μM) was found to be the most active compound against AChE, and 1-(4-fluorophenyl)-3-(4-(6-nitro-2-oxo-2H-chromen-3-yl)thiazol-2-yl)urea (e31) exhibited the strongest inhibition against BuChE with IC50 value of 4.93 μM, which was 3.5-fold more potent than that of galantamine. The selectivity of f8 and e31 were 2.64 and 0.04, respectively. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were investigated for antioxidant activity. Among them, f8, f4 and f6 (IC50=1.64, 1.82 and 2.69 μM, respectively) showed significantly better ABTS cation radical scavenging ability than standard quercetin (IC50 = 15.49 μM).
    MeSH term(s) Acetylcholinesterase/metabolism ; Animals ; Antioxidants/chemical synthesis ; Antioxidants/chemistry ; Antioxidants/pharmacology ; Butyrylcholinesterase/metabolism ; Cholinesterase Inhibitors/chemical synthesis ; Cholinesterase Inhibitors/chemistry ; Cholinesterase Inhibitors/pharmacology ; Coumarins/chemical synthesis ; Coumarins/chemistry ; Coumarins/pharmacology ; Electrophorus ; Horses ; Structure-Activity Relationship ; Thiazoles/chemical synthesis ; Thiazoles/chemistry ; Thiazoles/pharmacology ; Urea/analogs & derivatives ; Urea/chemical synthesis ; Urea/pharmacology
    Chemical Substances Antioxidants ; Cholinesterase Inhibitors ; Coumarins ; Thiazoles ; Urea (8W8T17847W) ; Acetylcholinesterase (EC 3.1.1.7) ; Butyrylcholinesterase (EC 3.1.1.8)
    Language English
    Publishing date 2015-04
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2015.02.002
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 4207: Show issues Location:
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  4. Article ; Online: New saccharin derivatives as tyrosinase inhibitors.

    Gençer, Nahit / Demir, Dudu / Sonmez, Fatih / Kucukislamoglu, Mustafa

    Bioorganic & medicinal chemistry

    2012  Volume 20, Issue 9, Page(s) 2811–2821

    Abstract: A newly series of 6-(phenylurenyl/thiourenyl) saccharin (6a-y) derivatives were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated. A 70-fold purification of the enzyme with 6.85% yield was achieved ... ...

    Abstract A newly series of 6-(phenylurenyl/thiourenyl) saccharin (6a-y) derivatives were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated. A 70-fold purification of the enzyme with 6.85% yield was achieved by using a Sepharose 4B-l-tyrosine-p-amino benzoic acid affinity column. The result showed that all the synthesized compounds inhibited the tyrosinase enzyme activity. Among the compounds synthesized, 6-(3-iodophenylthiourenyl) saccharin (6s) was found to be most active one (K(i)=3.95 μM) and the inhibition kinetics analyzed by Lineweaver-Burk double reciprocal plots revealed that compound 6s was a competitive inhibitor. Structure-activity relationships study showed that generally, most of the 6-(phenylthiourenyl) saccharin derivatives (6m-y) exhibited higher inhibitory activity than 6-(phenylurenyl) saccharin derivatives (6a-l). An electron-withdrawing group at 3-position of phenylurenyl-ring increased in activity and the halogen series at 3-position of phenylthiourenyl-ring showed a qualitative relationship for higher inhibitory activity with increasing size and polarizability. We also calculated HOMO-LUMO energy levels and dipole moments of some selected the synthesized compounds (6a, 6h, 6m and 6s) using Gaussian software.
    MeSH term(s) Enzyme Activation/drug effects ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Kinetics ; Monophenol Monooxygenase/antagonists & inhibitors ; Monophenol Monooxygenase/metabolism ; Musa/enzymology ; Quantum Theory ; Saccharin/chemical synthesis ; Saccharin/chemistry ; Software ; Structure-Activity Relationship
    Chemical Substances Enzyme Inhibitors ; Monophenol Monooxygenase (EC 1.14.18.1) ; Saccharin (FST467XS7D)
    Language English
    Publishing date 2012-05-01
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2012.03.033
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    Zs.A 3815: Show issues Location:
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  5. Article ; Online: Synthesis, structure-activity relationships and biological activity of new isatin derivatives as tyrosinase inhibitors.

    Gencer, Nahit / Sonmez, Fatih / Demir, Dudu / Arslan, Oktay / Kucukislamoglu, Mustafa

    Current topics in medicinal chemistry

    2014  Volume 14, Issue 12, Page(s) 1450–1462

    Abstract: A newly series of isatin derivatives (6a-t) containing alkyl/aryl urea groups were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated. Tyrosinase was purified from banana on an affinity gel comprised ... ...

    Abstract A newly series of isatin derivatives (6a-t) containing alkyl/aryl urea groups were synthesized and their inhibitory effects on the diphenolase activity of banana tyrosinase were evaluated. Tyrosinase was purified from banana on an affinity gel comprised of Sepharose 4B-L-tyrosine-p-aminobenzoic acid. The results showed that all the synthesized compounds inhibited the tyrosinase enzyme activity. Among them, 1-(2,3-dioxoindolin-5-yl)-3-(4-nitrophenyl)urea (6l) was found to be most active compound (Ki = 24.96 µM). The inhibition kinetics was analysed by Lineweaver-Burk double reciprocal plots. It revealed that compound 6l was a competitive inhibitor. According to results of structure-activity relationship, generally, the compounds electron-donating group bonded to the phenyl ring have higher inhibitory activity against tyrosinase than halogen group bonded to the phenyl ring. The inhibitory activities of alkyl urea substituted compounds decreased with increasing carbon number of the alkyl groups at urea moiety. The halogen series at the para position of the phenyl ring showed a qualitative relationship for higher inhibitory activity with increasing size and polarizability. HOMOLUMO energy levels and dipole moments of some selected compounds (6a, 6d, 6h, 6l and 6o) were also calculated by Gaussian software.
    MeSH term(s) Dose-Response Relationship, Drug ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Isatin/analogs & derivatives ; Isatin/chemical synthesis ; Isatin/chemistry ; Isatin/pharmacology ; Molecular Structure ; Monophenol Monooxygenase/antagonists & inhibitors ; Monophenol Monooxygenase/metabolism ; Quantum Theory ; Structure-Activity Relationship
    Chemical Substances Enzyme Inhibitors ; Isatin (82X95S7M06) ; Monophenol Monooxygenase (EC 1.14.18.1)
    Language English
    Publishing date 2014-05-28
    Publishing country United Arab Emirates
    Document type Journal Article
    ZDB-ID 2064823-6
    ISSN 1873-4294 ; 1568-0266
    ISSN (online) 1873-4294
    ISSN 1568-0266
    DOI 10.2174/1568026614666140530104344
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 5572: Show issues Location:
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  6. Article ; Online: Design, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors.

    Sonmez, Fatih / Zengin Kurt, Belma / Gazioglu, Isil / Basile, Livia / Dag, Aydan / Cappello, Valentina / Ginex, Tiziana / Kucukislamoglu, Mustafa / Guccione, Salvatore

    Journal of enzyme inhibition and medicinal chemistry

    2017  Volume 32, Issue 1, Page(s) 285–297

    Abstract: New coumaryl-thiazole derivatives with the acetamide moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and in vitro tested as acetylcholinesterase (AChE) inhibitors. 2-(diethylamino)-N-(4-(2-oxo-2H-chromen-3-yl) ... ...

    Abstract New coumaryl-thiazole derivatives with the acetamide moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and in vitro tested as acetylcholinesterase (AChE) inhibitors. 2-(diethylamino)-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)acetamide (6c, IC
    MeSH term(s) Acetylcholinesterase/drug effects ; Animals ; Cell Line, Tumor ; Cholinesterase Inhibitors/pharmacology ; Coumarins/pharmacology ; Drug Design ; Kinetics ; Ligands ; Molecular Docking Simulation ; Spectrum Analysis/methods
    Chemical Substances Cholinesterase Inhibitors ; Coumarins ; Ligands ; Acetylcholinesterase (EC 3.1.1.7)
    Language English
    Publishing date 2017-01-12
    Publishing country England
    Document type Journal Article
    ZDB-ID 2082578-X
    ISSN 1475-6374 ; 1475-6366
    ISSN (online) 1475-6374
    ISSN 1475-6366
    DOI 10.1080/14756366.2016.1250753
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 3004: Show issues Location:
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  7. Article ; Online: Synthesis, biological activity and multiscale molecular modeling studies for coumaryl-carboxamide derivatives as selective carbonic anhydrase IX inhibitors.

    Zengin Kurt, Belma / Sonmez, Fatih / Durdagi, Serdar / Aksoydan, Busecan / Ekhteiari Salmas, Ramin / Angeli, Andrea / Kucukislamoglu, Mustafa / Supuran, Claudiu T

    Journal of enzyme inhibition and medicinal chemistry

    2017  Volume 32, Issue 1, Page(s) 1042–1052

    Abstract: New coumaryl-carboxamide derivatives with the thiourea moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and their inhibitory activity against the human carbonic anhydrase (hCA) isoforms hCA I, II, VII and IX ... ...

    Abstract New coumaryl-carboxamide derivatives with the thiourea moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and their inhibitory activity against the human carbonic anhydrase (hCA) isoforms hCA I, II, VII and IX were evaluated. While the hCA I, II and VII isoforms were not inhibited by the investigated compounds, the tumour-associated isoform hCA IX was inhibited in the high nanomolar range. 2-Oxo-N-((2-(pyrrolidin-1-yl)ethyl)carbamothioyl)-2H-chromene-3-carboxamide (e11) exhibited a selective inhibitory action against hCA IX with the K
    MeSH term(s) Algorithms ; Carbonic Anhydrase IX/antagonists & inhibitors ; Carbonic Anhydrase IX/metabolism ; Carbonic Anhydrase Inhibitors/chemical synthesis ; Carbonic Anhydrase Inhibitors/chemistry ; Carbonic Anhydrase Inhibitors/pharmacology ; Coumaric Acids/chemical synthesis ; Coumaric Acids/chemistry ; Coumaric Acids/pharmacology ; Dose-Response Relationship, Drug ; Humans ; Models, Molecular ; Molecular Structure ; Structure-Activity Relationship ; Thiourea/chemistry ; Thiourea/pharmacology
    Chemical Substances Carbonic Anhydrase Inhibitors ; Coumaric Acids ; Carbonic Anhydrase IX (EC 4.2.1.1) ; Thiourea (GYV9AM2QAG)
    Language English
    Publishing date 2017-12
    Publishing country England
    Document type Journal Article
    ZDB-ID 2082578-X
    ISSN 1475-6374 ; 1475-6366
    ISSN (online) 1475-6374
    ISSN 1475-6366
    DOI 10.1080/14756366.2017.1354857
    Database MEDical Literature Analysis and Retrieval System OnLINE

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

    Sonmez, Fatih / Bilen, Cigdem / Sumersan, Sinem / Gencer, Nahit / Isik, Semra / Arslan, Oktay / Kucukislamoglu, Mustafa

    Journal of enzyme inhibition and medicinal chemistry

    2014  Volume 29, Issue 1, Page(s) 118–123

    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 ...

    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.
    MeSH term(s) Carbonic Anhydrase I/metabolism ; Carbonic Anhydrase II/metabolism ; Erythrocytes/enzymology ; In Vitro Techniques ; Saccharin/chemistry ; Structure-Activity Relationship
    Chemical Substances Carbonic Anhydrase I (EC 4.2.1.-) ; Carbonic Anhydrase II (EC 4.2.1.-) ; Saccharin (FST467XS7D)
    Language English
    Publishing date 2014-02
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2082578-X
    ISSN 1475-6374 ; 1475-6366
    ISSN (online) 1475-6374
    ISSN 1475-6366
    DOI 10.3109/14756366.2012.757222
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Synthesis and in vitro inhibition effect of new pyrido[2,3-d]pyrimidine derivatives on erythrocyte carbonic anhydrase I and II.

    Kuday, Hilal / Sonmez, Fatih / Bilen, Cigdem / Yavuz, Emre / Gençer, Nahit / Kucukislamoglu, Mustafa

    BioMed research international

    2014  Volume 2014, Page(s) 594879

    Abstract: In vitro inhibition effects of indolylchalcones and new pyrido[2,3-d]pyrimidine derivatives on purified human carbonic anhydrase I and II (hCA I and II) were investigated by using CO2 as a substrate. The results showed that all compounds inhibited the ... ...

    Abstract In vitro inhibition effects of indolylchalcones and new pyrido[2,3-d]pyrimidine derivatives on purified human carbonic anhydrase I and II (hCA I and II) were investigated by using CO2 as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among all the synthesized compounds, 7e (IC50 = 6.79 µM) was found to be the most active compound for hCA I inhibitory activity and 5 g (IC50 = 7.22 µM) showed the highest hCA II inhibitory activity. Structure-activity relationships study showed that indolylchalcone derivatives have higher inhibitory activities than pyrido[2,3-d]pyrimidine derivatives on hCA I and hCA II. Additionally, methyl group bonded to uracil ring increases inhibitory activities on both hCA I and hCA II.
    MeSH term(s) Carbon Dioxide/chemistry ; Carbonic Anhydrase I/antagonists & inhibitors ; Carbonic Anhydrase I/chemistry ; Carbonic Anhydrase I/metabolism ; Carbonic Anhydrase II/antagonists & inhibitors ; Carbonic Anhydrase II/chemistry ; Carbonic Anhydrase II/metabolism ; Chalcone/administration & dosage ; Chalcone/chemical synthesis ; Erythrocytes/enzymology ; Healthy Volunteers ; Humans ; Pyrimidines/administration & dosage ; Pyrimidines/chemical synthesis ; Structure-Activity Relationship
    Chemical Substances Pyrimidines ; Carbon Dioxide (142M471B3J) ; Chalcone (5S5A2Q39HX) ; Carbonic Anhydrase I (EC 4.2.1.-) ; Carbonic Anhydrase II (EC 4.2.1.-)
    Language English
    Publishing date 2014-08-04
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2698540-8
    ISSN 2314-6141 ; 2314-6133
    ISSN (online) 2314-6141
    ISSN 2314-6133
    DOI 10.1155/2014/594879
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Synthesis, antioxidant and carbonic anhydrase I and II inhibitory activities of novel sulphonamide-substituted coumarylthiazole derivatives.

    Kurt, Belma Zengin / Sönmez, Fatih / Bilen, Çiğdem / Ergun, Adem / Gençer, Nahit / Arslan, Oktay / Kucukislamoglu, Mustafa

    Journal of enzyme inhibition and medicinal chemistry

    2016  Volume 31, Issue 6, Page(s) 991–998

    Abstract: New secondary benzenesulphonamide-substituted coumarylthiazole derivatives were synthesized and their inhibitory effects on purified carbonic anhydrase I and II were evaluated using CO2 as a substrate. The result showed that all the synthesized compounds ...

    Abstract New secondary benzenesulphonamide-substituted coumarylthiazole derivatives were synthesized and their inhibitory effects on purified carbonic anhydrase I and II were evaluated using CO2 as a substrate. The result showed that all the synthesized compounds exhibited inhibitory activity on both hCA I and hCA II with N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)naphthalene-2-sulphonamide (5f, IC50 value of 5.63 and 8.48 µM, against hCA I and hCA II, respectively) as the strongest inhibitor revealed from this study. Structure-activity relationship revealed that the inhibitory activity of the synthesized compounds is related to the type of the halogen and bulky substituent on the phenyl ring. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. 4-methoxy-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)benzenesulphonamide (5e) exhibited the strongest ABTS and CUPRAC activity with IC50 value of 48.83 µM and A0.50 value of 23.29 µM, respectively.
    MeSH term(s) Antioxidants/chemical synthesis ; Antioxidants/chemistry ; Antioxidants/pharmacology ; Carbonic Anhydrase I/antagonists & inhibitors ; Carbonic Anhydrase I/metabolism ; Carbonic Anhydrase II/antagonists & inhibitors ; Carbonic Anhydrase II/metabolism ; Carbonic Anhydrase Inhibitors/chemical synthesis ; Carbonic Anhydrase Inhibitors/chemistry ; Carbonic Anhydrase Inhibitors/pharmacology ; Dose-Response Relationship, Drug ; Humans ; Molecular Structure ; Structure-Activity Relationship ; Sulfonamides/chemistry ; Sulfonamides/pharmacology ; Thiazoles/chemical synthesis ; Thiazoles/chemistry ; Thiazoles/pharmacology
    Chemical Substances Antioxidants ; Carbonic Anhydrase Inhibitors ; Sulfonamides ; Thiazoles ; Carbonic Anhydrase I (EC 4.2.1.-) ; Carbonic Anhydrase II (EC 4.2.1.-)
    Language English
    Publishing date 2016-12
    Publishing country England
    Document type Journal Article
    ZDB-ID 2082578-X
    ISSN 1475-6374 ; 1475-6366
    ISSN (online) 1475-6374
    ISSN 1475-6366
    DOI 10.3109/14756366.2015.1077823
    Database MEDical Literature Analysis and Retrieval System OnLINE

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