Discovery of potent carbonic anhydrase,acetylcholinesterase, and butyrylcholinesterase enzymes inhibitors: The new amides and thiazolidine‐4‐ones synthesized on an acetophenone base |
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| Authors: | Parham Taslimi Sabiya Osmanova ?lhami Gulçin Sabira Sardarova Vagif Farzaliyev Afsun Sujayev Ruya Kaya Fatma Koc Sukru Beydemir Saleh H Alwasel Omer Irfan Kufrevioglu |
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| Affiliation: | 1. Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey;2. Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan;3. Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia;4. Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eski?ehir, Turkey |
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| Abstract: | Compounds containing nitrogen and sulfur atoms can be widely used in various fields, including industry, medicine, biotechnology, and chemical technology. Among them, amides of acids and heterocyclic compounds have an important place. These amides and thiazolidine‐4‐ones showed good inhibitory action against butyrylcholinesterase (BChE), acetylcholinesterase (AChE), and human carbonic anhydrase isoforms. AChE exists at high concentrations in the brain and red blood cells. BChE is an important enzyme that is plentiful in the liver, and it is released into the blood in a soluble form. They were demonstrated to have effective inhibition profiles with Ki values of 23.76–102.75 nM against hCA I, 58.92–136.64 nM against hCA II, 1.40–12.86 nM against AChE, and 9.82–52.77 nM against BChE. On the other hand, acetazolamide showed Ki value of 482.63 ± 56.20 nM against hCA I, and 1019.60 ± 163.70 nM against hCA II. Additionally, Tacrine inhibited AChE and BChE, showing Ki values of 397.03 ± 31.66 and 210.21 ± 15.98 nM, respectively. |
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| Keywords: | acetophenone acetylcholinesterase butyrylcholinesterase carbonic anhydrase enzyme inhibition |
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