Microwave assisted synthesis of novel hybrid tacrine-sulfonamide derivatives and investigation of their antioxidant and anticholinesterase activities |
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| Institution: | 1. Department of Chemistry, College of Science, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;2. Basic and Applied Scientific Research Center, College of science, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia;3. Department of Chemistry, College of Science, King Khalid University, P.O. Box 9004, Abha, 61413, Saudi Arabia;4. Department of Biology, College of Science, King Khalid University, P.O. Box 9004, Abha, 61413, Saudi Arabia;5. Depatment of Chemistry, Hazara University, Khyber Pakhtunkhwa, Mansehra, 21300, Pakistan;6. Department of Chemistry, University of Okara, Okara, 56130, Pakistan;7. Department of Zoology, Faculty of life sciences, University of Okara, Okara, 56130, Pakistan;8. Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan, 23200, Pakistan |
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| Abstract: | A novel series of tacrine derivatives containing sulfonamide group were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized tacrine-sulfonamides (VIIIa–o) exhibited inhibitory activity on both cholinesterases. VIIIg showed the highest inhibitory activity on AChE IC50 = 0.009 μM. This value is 220-fold greater than that of galantamine (IC50 = 2.054 μM) and 6-fold greater than tacrine (IC50 = 0.055 μM). VIIIf displayed the strongest inhibition of BuChE (IC50 = 2.250 μM), which is close to donepezil (IC50 = 2.680 μM) and 8-fold greater than that of galantamine (IC50 = 18.130 μM) Furthermore, all of the synthesized tacrine derivatives showed higher inhibition of BuChE than that of galantamine. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were investigated for the antioxidant activity. Among them, VIIIb (IC50 = 94.390 ± 2.310 μM) showed significantly better ABTS cation radical scavenging ability than all of the new synthesized compounds. |
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| Keywords: | Tacrine Sulfonamide Chromene AChE BuChE Antioxidant |
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