Synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory potential of hydrazide based Schiff bases |
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| Institution: | 1. Department of Chemistry, Hazara University, Mansehra 21300, Pakistan;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, UiTM, 40450 Shah Alam, Selangor, Malaysia;4. Department of Biohemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;5. Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;6. Center for Advanced Drug Research, COMSATS Institute of Information Technology, University Road, Abbottabad 22060, KPK, Pakistan;7. Department of Biochemistry, Hazara University, Mansehra 21300, Pakistan;8. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;1. Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpa?a, 34668, ?stanbul, Turkey;2. Rutgers-New Jersey Medical School, Department of Microbiology, Biochemistry and Molecular Genetics, Newark, NJ 07103, USA;3. Bilkent University, Department of Molecular Biology and Genetics, 06800, Bilkent Ankara, Turkey;4. Cancer Systems Biology Laboratory, Graduate School of Informatics Middle East Technical University, ODTU, 06800, Ankara, Turkey;1. Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D. E., Malaysia;2. Faculty of Applied Science, UiTM Shah Alam, 40450 Shah Alam, Selangor D.E., Malaysia;3. Department of Chemistry, Abdul Wali Khan University Mardan, Khyber Pakhtunkhwa, Pakistan;4. Department of Chemistry, Hazara University Mansehra, 21300 Khyber Pakhtunkhwa, Pakistan;5. Department of Bioinformatics, Quaide-e-Azam University, Islamabad, Pakistan;1. Recep Tayyip Erdogan University, Faculty of Arts and Sciences, Department of Chemistry 53100 Rize, Turkey;2. Recep Tayyip Erdogan University, Education Faculty, 53200 Rize, Turkey;3. Agri Ibrahim Cecen University, Pharmacy Faculty, 04100 Agri, Turkey;1. Department of Chemistry, Hazara University, Mansehra 21120, Pakistan;2. Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia;3. Faculty of Applied Science, Universiti Teknologi MARA, 40450 Shah Alam, Malaysia;4. Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;5. Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan;6. HEJ, Research Institute of Chemistry, ICCBS, University of Karachi, Karachi 75270, Pakistan |
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| Abstract: | To discover multifunctional agents for the treatment of Alzheimer’s disease, a series of hydrazide based Schiff bases were designed and synthesized based on multitarget-directed strategy. We have synthesized twenty-eight analogs of hydrazide based Schiff bases, characterized by various spectroscopic techniques and evaluated in vitro for acetylcholinesterase and butyrylcholinesterase inhibition. All compounds showed varied degree of acetylcholinesterase and butyrylcholinesterase inhibition when compared with standard Eserine. Among the series, compounds 10, 3 and 24 having IC50 values 4.12 ± 0.01, 8.12 ± 0.01 and 8.41 ± 0.06 μM respectively showed potent acetylcholinesterase inhibition when compared with Eserine (IC50 = 0.85 ± 0.0001 μM). Three compounds 13, 24 and 3 having IC50 values 6.51 ± 0.01, 9.22 ± 0.07 and 37.82 ± 0.14 μM respectively showed potent butyrylcholinesterase inhibition by comparing with eserine (IC50 = 0.04 ± 0.0001 μM). The remaining compounds also exhibited moderate to weak inhibitory potential. Structure activity relationship has been established. Through molecular docking studies the binding interaction was confirmed. |
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| Keywords: | Synthesis Acetylcholinesterase Butyrylcholinesterase Molecular docking Schiff bases SAR |
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