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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.
Bioorg Chem. 2019 05; 86:705-713.BC

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.

Authors+Show Affiliations

Recep Tayyip Erdogan University, Faculty of Arts and Sciences, Department of Chemistry 53100 Rize, Turkey. Electronic address: musa.ozil@erdogan.edu.tr.Recep Tayyip Erdogan University, Education Faculty, 53200 Rize, Turkey.Agri Ibrahim Cecen University, Pharmacy Faculty, 04100 Agri, Turkey.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

30836234

Citation

Özil, Musa, et al. "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." Bioorganic Chemistry, vol. 86, 2019, pp. 705-713.
Özil M, Balaydın HT, Şentürk M. 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. Bioorg Chem. 2019;86:705-713.
Özil, M., Balaydın, H. T., & Şentürk, M. (2019). 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. Bioorganic Chemistry, 86, 705-713. https://doi.org/10.1016/j.bioorg.2019.02.045
Özil M, Balaydın HT, Şentürk M. 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. Bioorg Chem. 2019;86:705-713. PubMed PMID: 30836234.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 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. AU - Özil,Musa, AU - Balaydın,Halis Türker, AU - Şentürk,Murat, Y1 - 2019/02/22/ PY - 2018/11/18/received PY - 2019/02/12/revised PY - 2019/02/21/accepted PY - 2019/3/6/pubmed PY - 2020/4/1/medline PY - 2019/3/6/entrez KW - 1,2,4-Triazole KW - Benzohydrazide KW - Carbonic anhydrase KW - Cholinesterase KW - Enzyme inhibition KW - Schiff base SP - 705 EP - 713 JF - Bioorganic chemistry JO - Bioorg. Chem. VL - 86 N2 - 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. SN - 1090-2120 UR - https://www.unboundmedicine.com/medline/citation/30836234/Synthesis_of_5_methyl_24_dihydro_3H_124_triazole_3_one's_aryl_Schiff_base_derivatives_and_investigation_of_carbonic_anhydrase_and_cholinesterase__AChE_BuChE__inhibitory_properties_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0045-2068(18)31343-9 DB - PRIME DP - Unbound Medicine ER -