Design,and facile synthesis of 1,3 diaryl-3-(arylamino)propan-1-one derivatives as the potential alpha-amylase inhibitors and antioxidants |
| |
| Institution: | 1. Department of Pharmaceutical Chemistry, Kabul University, Kabul, Afghanistan;2. Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, India;1. Department of Metallurgical and Materials Engineering, Indian Institute of Technology Roorkee-247667, India;2. School of Electronics & Electrical Engineering, Lovely Professional University, Punjab-144411,India;1. Department of Chemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan;2. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;3. Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;4. Monash University School of Chemical Engineering, Bandar Subway, 47500 Selangor Alam Campus, 42300, Malaysia;5. Department of Biochemistry, Hazara University, Mansehra 21300, Khyber Pakhtunkhwa, Pakistan;6. Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA Cawangan Selangor Kampus Puncak Alam, 42300 Bandar Puncak Alam, Selangor D. E., Malaysia.;7. Faculty of Pharmacy, Universiti Teknologi MARA Cawangan Selangor Kampus Puncak Alam, 42300 Bandar Puncak Alam, Selangor D. E., Malaysia;8. Department of Chemistry, University of Karachi, Karachi 75270, Pakistan;9. Department of Computer Information Systems, College of Computer Science & Information Technology (CCSIT), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;1. Chemical Science and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, India;2. Academy of Scientific and Innovative Research (AcSIR), Thiruvananthapuram 695019, India;3. Agroprocessing and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, India;4. Centre for Computational Modeling and Data Engineering, Indian Institute of Information Technology and Management, Thiruvananthapuram 695581, India;5. Phytochemistry Division, Jawaharlal Nehru Tropical Botanic Garden and Research Institute, Palode, Thiruvananthapuram 695562, India;1. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;2. Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia;3. Faculty of Applied Science, Universiti Teknologi MARA, 40450 Shah Alam, Selangor D. E, Malaysia;4. Department of Chemistry, COMSATS Institute of Information Technology, University Road, Abbottabad 22060, KPK, Pakistan;5. Department of Chemistry, Hazara University, Mansehra 21300, Pakistan;6. Monash University School of Chemical Engineering, Bandar Subway 47500, Selangor, Malaysia;7. Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Buraidah 51452, Saudi Arabia;8. Department of Nano-Medicine Research, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;9. Deanship of Scientific Research, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;10. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, AIMST University, Semeling, Bedong 08100, Malaysia;1. Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara, Punjab 144411, India;2. Department of Pharmacology & Toxicology, National Institute of Pharmaceutical Education and Research, S.A.S. Nagar, Mohali, Punjab 160062, India;3. Department of Biotechnology, School of Bioscience, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara, Punjab 144411, India;4. Department of Pharmacology, School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara, Punjab 144411, India |
| |
| Abstract: | Diabetes is the most prevalent metabolic disorder causing a high rate of mortality and morbidity. Recently alpha-amylase is reported to be good drug design target for the treatment of diabetes mellitus. We have designed 116 molecules based on aza-Michael adduct of trans-chalcone as 1,3 diaryl-3-(arylamino)propan-1-ones which were studied by molecular docking and among them best six derivatives were synthesized easily via aza-Michael addition on trans-chalcone using KOH as a catalyst and evaluated for alpha-amylase inhibition along with antioxidant activity. It was observed that all compounds have alpha-amylase inhibitory activity but at different extents. The molecule 3e is the most potent alpha-amylase inhibitor of this series. 3a is the second most potent compound, whereas only one molecule 3d has shown antioxidant activity. |
| |
| Keywords: | Diabetes Antidiabetic Alpha-amylase inhibitor Aza-Michael addition Antioxidant |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
