Synthesis of 5-methyl-2,4-dihydro-3H-1,2,4-triazole-3-one’s aryl Schiff base derivatives and investigation of carbonic anhydrase and cholinesterase (AChE,BuChE) inhibitory properties |
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| Institution: | 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. Balikesir University, Science & Art Faculty, Department of Chemistry, Balikesir, Turkey;2. University of Florence, Neurofarba Department, Via Ugo Schiff 6, Polo Scientifico, 50019 Sesto Fiorentino, Firenze, Italy;3. Department of Biophysics, School of Medicine, Bahcesehir University, Istanbul, Turkey;4. Ondokuz May?s University, Department of Agricultural Biotechnology, 55139 Samsun, Turkey;5. Agri Ibrahim Cecen University, Department of Chemistry, 04100 Agri, Turkey;6. Bingol University, Faculty of Art & Science, Department of Chemistry, 12000 Bingol, Turkey;7. A?r? ?brahim Çeçen University, School of Heatlh Services, 04100 A?r?, Turkey;1. Technical Sciences Vocational School, Giresun University, 28049 Giresun, Turkey;2. A?r? ?brahim Çeçen University, Department of Pharmaceutical Technology, 04100 A?r?, Turkey;3. A?r? ?brahim Çeçen University, Science and Art Faculty, Chemistry Department, 04100 A?r?, Turkey;4. Universitá degli Studi di Firenze, Dipartimento Neurofarba, Sezione di Scienze, Polo Scientifico, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;1. Department of Physics, T.K.M. College of Arts and Science, Karicode, Kollam, Kerala, 691 005, India;2. Laboratory of Medicinal Chemistry, Faculty of Medicine and Pharmacy, University Mohammed V, Rabat, Morocco;3. Physicochemical Service, Drugs Quality Control Laboratory, Division of Drugs and Pharmacy, Ministry of Health, 10100, Rabat, Morocco;4. Laboratory of Pharmacology and Toxicology, Pharmacokinetic Research Team, Faculty of Medicine and Pharmacy, University Mohammed V, Rabat, Morocco;5. University of Novi Sad, Faculty of Sciences, Department of Physics, Trg D. Obradovi?a 4, 21000, Novi Sad, Serbia;6. University of Novi Sad, Faculty of Sciences, Department of Chemistry, Biochemistry and Environmental Protection, Trg D. Obradovi?a 3, 21000, Novi Sad, Serbia;7. LCAE, Department of Chemistry, Faculty of Sciences, University Mohamed I, Oujda, Morocco;1. Depatment of Chemistry, Hazara University, Mansehra 21300, Pakistan;2. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 3144, Saudi Arabia;3. Department of Biochemistry, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan;4. Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor D.E., Malaysia;5. H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;1. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India;2. Department of Regulatory Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India;1. College of Pharmacy, Shaanxi University of Chinese Medicine, Xi’an/Xianyang, China;2. Department of Chemistry, Hong Kong University of Science and Technology, Hong Kong, China;3. College of Biology Pharmacy and Food Engineering, Shangluo University, Shangluo, China;4. School of Chemical Engineering, Northwest University, Xi’an, China;5. School of Chemistry and Materials, Northwest University, Xi’an, China;6. Department of Medcine, Ankang Vocational and Technical College, Ankang, China;7. State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), College of Chemistry, Nankai University, Tianjin, China |
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| Abstract: | Carbonic anhydrase enzymes (EC 4.2.1.1, CAs) are metalloenzyme families that catalyze the rapid conversion of H2O and CO2 to HCO3– and H+. CAs are found in different tissues where they participate in various significant biochemical processes such as ion transport, carbon dioxide respiration, ureagenesis, lipogenesis, bone resorption, electrolyte secretion, acid-base balance, and gluconeogenesis. In such processes, many CAs are significant therapeutic targets because of their inhibitory potentials especially in the treatment of some diseases such as edema, glaucoma, obesity, cancer, epilepsy, and osteoporosis. Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) inhibitors are also valuable compounds for different therapeutic applications including Alzheimer’s disease. In this work, we report a fast and effective synthesis of 5-methyl-2,4-dihydro-3H-1,2,4-triazole-3-one’s aryl Schiff base derivatives and also their CA and cholinesterases inhibitory properties. Our findings showed that these Schiff base derivatives, with triazole ring, found as strong CA and cholinesterases inhibitors. |
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| Keywords: | 1 2 4-Triazole Schiff base Benzohydrazide Carbonic anhydrase Cholinesterase Enzyme inhibition |
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