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  1. Article ; Online: Design and synthesis of phenoxy methyl-oxadiazole compounds against Alzheimer's disease.

    Evren, Asaf E / Nuha, Demokrat / Özkan, Begüm N S / Kahraman, Çiğdem / Gönülalan, Ekrem M / Yurttaş, Leyla

    Archiv der Pharmazie

    2024  , Page(s) e2400115

    Abstract: This study examines the synthesis and evaluation of 11 newly developed compounds as potential anti-Alzheimer's agents that occur via cholinesterase and β-secretase inhibition. The compounds were tested for their inhibitory activity against ... ...

    Abstract This study examines the synthesis and evaluation of 11 newly developed compounds as potential anti-Alzheimer's agents that occur via cholinesterase and β-secretase inhibition. The compounds were tested for their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using the modified Ellman method. The results showed that several compounds exhibited significant inhibition of AChE, particularly compounds 6d, 7a, and 7e, which demonstrated high inhibitory activity at lower concentrations, with IC
    Language English
    Publishing date 2024-04-24
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 6381-2
    ISSN 1521-4184 ; 0365-6233 ; 1437-1014
    ISSN (online) 1521-4184
    ISSN 0365-6233 ; 1437-1014
    DOI 10.1002/ardp.202400115
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Novel oxadiazole-thiadiazole derivatives: synthesis, biological evaluation, and

    Evren, Asaf Evrim / Nuha, Demokrat / Dawbaa, Sam / Karaduman, Abdullah Burak / Sağlik, Begüm Nurpelin / Yurttaş, Leyla

    Journal of biomolecular structure & dynamics

    2023  , Page(s) 1–13

    Abstract: In the search for new anticancer agents, we synthesized a new series of thiazole derivatives carried on thiadiazole-oxadiazole hybrid. Final compounds ( ...

    Abstract In the search for new anticancer agents, we synthesized a new series of thiazole derivatives carried on thiadiazole-oxadiazole hybrid. Final compounds (
    Language English
    Publishing date 2023-08-17
    Publishing country England
    Document type Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2023.2247087
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 2093: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
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  3. Article ; Online: New

    Dawbaa, Sam / Türkeş, Cüneyt / Nuha, Demokrat / Demir, Yeliz / Evren, Asaf Evrim / Yurttaş, Leyla / Beydemir, Şükrü

    Journal of biomolecular structure & dynamics

    2024  , Page(s) 1–19

    Abstract: Various carbonic anhydrase (CA) enzyme isoforms are known today. In addition to the use of CA inhibitors as diuretics, antiepileptics and antiglaucoma agents, the inhibition of other specific isoforms of CA was reported to have clinical benefits in ... ...

    Abstract Various carbonic anhydrase (CA) enzyme isoforms are known today. In addition to the use of CA inhibitors as diuretics, antiepileptics and antiglaucoma agents, the inhibition of other specific isoforms of CA was reported to have clinical benefits in cancers. In this study, two groups of 1,3,4-thiadiazole derivatives were designed and synthesized to act as human CA I and II (
    Language English
    Publishing date 2024-03-27
    Publishing country England
    Document type Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2024.2331085
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 2093: Show issues Location:
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  4. Article ; Online: Synthesis of novel thiazolyl hydrazone derivatives as potent dual monoamine oxidase-aromatase inhibitors.

    Evren, Asaf Evrim / Nuha, Demokrat / Dawbaa, Sam / Sağlık, Begüm Nurpelin / Yurttaş, Leyla

    European journal of medicinal chemistry

    2022  Volume 229, Page(s) 114097

    Abstract: The inhibitory effects of 2-thiazolyl hydrazones on monoamine oxidase enzymes are known for a long time. In this study, a new series of 2-thiazolyl hydrazone derivatives were synthesized starting from 6-methoxy-2-naphthaldehyde. All of the synthesized ... ...

    Abstract The inhibitory effects of 2-thiazolyl hydrazones on monoamine oxidase enzymes are known for a long time. In this study, a new series of 2-thiazolyl hydrazone derivatives were synthesized starting from 6-methoxy-2-naphthaldehyde. All of the synthesized compounds were investigated in terms of their monoamine oxidase (MAO) inhibitory effects and significant results were found. The results showed that compound 2j potently inhibited MAO-A and MAO-B, while compound 2t strongly and selectively inhibited MAO-B compared to standard drugs. Compounds 2k and 2q exhibited selective and satisfying inhibition on MAO-B. In the aromatase inhibition studies of the compounds, it was determined that compounds 2q and 2u had high inhibitory properties. Molecular docking studies on MAO-A, MAO-B, and aromatase enzymes were carried out for the aforementioned compounds. Additionally, molecular dynamics simulation was studied for compound 2q on MAO-B and aromatase complexes. Finally, the Field-based QSAR study was developed and the structure-activity relationship (SAR) was explained. For the first time, dual inhibitors on MAO and aromatase enzyme were investigated together. The aim of this approach is for finding the potential agents that do not cause the cognitive disorders and may even treat neurodegenerative symptoms, thus, the aim was reached successfully.
    MeSH term(s) Aromatase/metabolism ; Aromatase Inhibitors/chemical synthesis ; Aromatase Inhibitors/pharmacology ; Drug Evaluation, Preclinical ; Humans ; Hydrazones/chemical synthesis ; Hydrazones/pharmacology ; Molecular Docking Simulation ; Monoamine Oxidase/metabolism ; Monoamine Oxidase Inhibitors/chemical synthesis ; Monoamine Oxidase Inhibitors/pharmacology ; Protein Binding ; Protein Conformation ; Structure-Activity Relationship
    Chemical Substances Aromatase Inhibitors ; Hydrazones ; Monoamine Oxidase Inhibitors ; Aromatase (EC 1.14.14.1) ; Monoamine Oxidase (EC 1.4.3.4)
    Language English
    Publishing date 2022-01-01
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2021.114097
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    Zs.B 784: Show issues Location:
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  5. Article ; Online: Synthesis, density functional theory calculation, molecular docking studies, and evaluation of novel 5-nitrothiophene derivatives for anticancer activity.

    Nuha, Demokrat / Evren, Asaf E / Çiyanci, Zennure Ş / Temel, Halide E / Akalin Çiftçi, Gülşen / Yurttaş, Leyla

    Archiv der Pharmazie

    2022  Volume 355, Issue 9, Page(s) e2200105

    Abstract: Within the scope of this study, new 2-{2-[(5-nitrothiophen-2-yl)methylene]hydrazinyl}thiazole derivatives (2a-j) were synthesized and investigated for their potential anticancer and enzyme inhibition activities. Spectroscopic techniques were used to ... ...

    Abstract Within the scope of this study, new 2-{2-[(5-nitrothiophen-2-yl)methylene]hydrazinyl}thiazole derivatives (2a-j) were synthesized and investigated for their potential anticancer and enzyme inhibition activities. Spectroscopic techniques were used to determine the structures of substances. The anticancer activities of compounds were detected in A549 human lung carcinoma and L929 murine fibroblast cell lines, determining cytotoxicity, apoptosis, mitochondrial membrane integrity, and caspase-3 activation. Compounds 2b bearing 4-nitrophenyl, 2c bearing phenyl, and 2d bearing 4-cyanophenyl moieties were specified with high anticancer activity, acting through an apoptotic pathway with an apoptosis ratio of 9.61%-15.59%. Mitochondrial membrane depolarization was determined to be 25.53% and 22.33% for compounds 2b and 2c, respectively. Furthermore, compound 2c exhibited excellent caspase-3 activation. A molecular docking study was realized with compound 2c on the caspase-3 enzyme. Furthermore, the electronic characteristics of the active compounds were investigated using density functional theory (DFT) at the B3LYP/6-31G (d, p) level. The frontier molecular orbital energy and atomic net charges were examined.
    MeSH term(s) Animals ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Caspase 3 ; Cell Line, Tumor ; Cell Proliferation ; Density Functional Theory ; Drug Screening Assays, Antitumor ; Humans ; Mice ; Molecular Docking Simulation ; Molecular Structure ; Structure-Activity Relationship
    Chemical Substances Antineoplastic Agents ; Caspase 3 (EC 3.4.22.-)
    Language English
    Publishing date 2022-05-18
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 6381-2
    ISSN 1521-4184 ; 0365-6233 ; 1437-1014
    ISSN (online) 1521-4184
    ISSN 0365-6233 ; 1437-1014
    DOI 10.1002/ardp.202200105
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

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    In stock of ZB MED Cologne/Königswinter

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