Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study
In this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as α-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by 1HNMR, 13CNMR, and EI-MS, and evaluated for α-amylase inhibition. Except compound...
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| Format: | Article |
| Language: | English |
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Wiley
2019-01-01
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| Series: | Heteroatom Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2019/7502347 |
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| author | Muhammad Taha Maryam Irshad Syahrul Imran Fazal Rahim Manikandan Selvaraj Noor Barak Almandil Ashik Mosaddik Sridevi Chigurupati Faisal Nawaz Nor Hadiani Ismail Mohamed Ibrahim |
| author_facet | Muhammad Taha Maryam Irshad Syahrul Imran Fazal Rahim Manikandan Selvaraj Noor Barak Almandil Ashik Mosaddik Sridevi Chigurupati Faisal Nawaz Nor Hadiani Ismail Mohamed Ibrahim |
| author_sort | Muhammad Taha |
| collection | DOAJ |
| description | In this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as α-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by 1HNMR, 13CNMR, and EI-MS, and evaluated for α-amylase inhibition. Except compound 11 all analogs showed α-amylase inhibitory activity with IC50 values from 1.709 ± 0.12 to 3.049 ± 0.25 μM against the standard acarbose (IC50 = 1.637 ± 0.153 μM). Compounds 1, 10, 14, and 20 exhibited outstanding inhibitory potential with IC50 value 1.763 ± 0.03, 1.747 ± 0.20, 1.709 ± 0.12, and 1.948 ± 0.23 μM, respectively, compared with the standard acarbose. Structure activity relationships have been established for the active compounds. To get an idea about the binding interaction of the compounds, molecular docking studies were done. |
| format | Article |
| id | doaj-art-61500c9c29b54ebba3b2f6a746b42a2e |
| institution | Kabale University |
| issn | 1042-7163 1098-1071 |
| language | English |
| publishDate | 2019-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Heteroatom Chemistry |
| spelling | doaj-art-61500c9c29b54ebba3b2f6a746b42a2e2025-02-03T05:58:55ZengWileyHeteroatom Chemistry1042-71631098-10712019-01-01201910.1155/2019/75023477502347Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking StudyMuhammad Taha0Maryam Irshad1Syahrul Imran2Fazal Rahim3Manikandan Selvaraj4Noor Barak Almandil5Ashik Mosaddik6Sridevi Chigurupati7Faisal Nawaz8Nor Hadiani Ismail9Mohamed Ibrahim10Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi ArabiaDepartment of Chemistry, University of Wah, Quaid Avenue, Wah Cantt 47000, PakistanAtta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, MalaysiaDepartment of Chemistry, Hazara University, Mansehra-21300, Khyber Pakhtunkhwa, PakistanSchool of Engineering, Monash University (Malaysia Campus), Bandar Sunway 47500, MalaysiaDepartment of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi ArabiaDepartment of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi ArabiaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Buraidah 51452, Saudi ArabiaDepartment of Chemistry, University of Wah, Quaid Avenue, Wah Cantt 47000, PakistanAtta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, MalaysiaDepartment of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi ArabiaIn this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as α-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by 1HNMR, 13CNMR, and EI-MS, and evaluated for α-amylase inhibition. Except compound 11 all analogs showed α-amylase inhibitory activity with IC50 values from 1.709 ± 0.12 to 3.049 ± 0.25 μM against the standard acarbose (IC50 = 1.637 ± 0.153 μM). Compounds 1, 10, 14, and 20 exhibited outstanding inhibitory potential with IC50 value 1.763 ± 0.03, 1.747 ± 0.20, 1.709 ± 0.12, and 1.948 ± 0.23 μM, respectively, compared with the standard acarbose. Structure activity relationships have been established for the active compounds. To get an idea about the binding interaction of the compounds, molecular docking studies were done.http://dx.doi.org/10.1155/2019/7502347 |
| spellingShingle | Muhammad Taha Maryam Irshad Syahrul Imran Fazal Rahim Manikandan Selvaraj Noor Barak Almandil Ashik Mosaddik Sridevi Chigurupati Faisal Nawaz Nor Hadiani Ismail Mohamed Ibrahim Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study Heteroatom Chemistry |
| title | Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study |
| title_full | Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study |
| title_fullStr | Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study |
| title_full_unstemmed | Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study |
| title_short | Thiazole Based Carbohydrazide Derivatives as α-Amylase Inhibitor and Their Molecular Docking Study |
| title_sort | thiazole based carbohydrazide derivatives as α amylase inhibitor and their molecular docking study |
| url | http://dx.doi.org/10.1155/2019/7502347 |
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