Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesteras...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2017-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/14756366.2016.1226298 |
| _version_ | 1818216448126877696 |
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| author | Zeynep Soyer Sirin Uysal Sulunay Parlar Ayse Hande Tarikogullari Dogan Vildan Alptuzun |
| author_facet | Zeynep Soyer Sirin Uysal Sulunay Parlar Ayse Hande Tarikogullari Dogan Vildan Alptuzun |
| author_sort | Zeynep Soyer |
| collection | DOAJ |
| description | A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman’s colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE. Among the tested compounds, compound 7 was found to be the most potent against AChE (IC50= 1.35 ± 0.08 μM), while compound 3 exhibited the highest inhibition against BuChE (IC50= 13.41 ± 0.62 μM). Molecular docking studies of the most active compound 7 in AChE showed that this compound can interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. |
| first_indexed | 2024-12-12T06:52:08Z |
| format | Article |
| id | doaj.art-4ea03bcd7b954ee28da24436fb4f7c31 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-12-12T06:52:08Z |
| publishDate | 2017-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-4ea03bcd7b954ee28da24436fb4f7c312022-12-22T00:34:03ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742017-01-01321131910.1080/14756366.2016.12262981226298Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitorsZeynep Soyer0Sirin Uysal1Sulunay Parlar2Ayse Hande Tarikogullari Dogan3Vildan Alptuzun4Ege UniversityEge UniversityEge UniversityEge UniversityEge UniversityA series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman’s colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE. Among the tested compounds, compound 7 was found to be the most potent against AChE (IC50= 1.35 ± 0.08 μM), while compound 3 exhibited the highest inhibition against BuChE (IC50= 13.41 ± 0.62 μM). Molecular docking studies of the most active compound 7 in AChE showed that this compound can interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE.http://dx.doi.org/10.1080/14756366.2016.1226298Acetylcholinesterase inhibitorbutyrylcholinesterase inhibitormolecular dockingphthalimidesulfonamide |
| spellingShingle | Zeynep Soyer Sirin Uysal Sulunay Parlar Ayse Hande Tarikogullari Dogan Vildan Alptuzun Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors Journal of Enzyme Inhibition and Medicinal Chemistry Acetylcholinesterase inhibitor butyrylcholinesterase inhibitor molecular docking phthalimide sulfonamide |
| title | Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors |
| title_full | Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors |
| title_fullStr | Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors |
| title_full_unstemmed | Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors |
| title_short | Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors |
| title_sort | synthesis and molecular docking studies of some 4 phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors |
| topic | Acetylcholinesterase inhibitor butyrylcholinesterase inhibitor molecular docking phthalimide sulfonamide |
| url | http://dx.doi.org/10.1080/14756366.2016.1226298 |
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