Synthesis and investigation of the conversion reactions of pyrimidine‐thiones with nucleophilic reagent and evaluation of their acetylcholinesterase,carbonic anhydrase inhibition,and antioxidant activities |
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| Authors: | Parham Taslimi Afsun Sujayev Fikret Turkan Emin Garibov Zübeyir Huyut Vagif Farzaliyev Sevgi Mamedova ?lhami Gulçin |
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| Institution: | 1. Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum 25240, Turkey;2. Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku 1029, Azerbaijan;3. Health Services Vocational School, Igd?r University, Igd?r 76000, Turkey;4. Department of Biochemistry, Faculty of Medical, Van Yuzuncu Yil University, Van 65090, Turkey |
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| Abstract: | The conversion reactions of pyrimidine‐thiones with nucleophilic reagent were studied during this scientific research. For this purpose, new compounds were synthesized by the interaction between 1,2‐epoxy propane, 1,2‐epoxy butane, and 4‐chlor‐1‐butanol and pyrimidine‐thiones. These pyrimidine‐thiones derivatives ( A–K ) showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase (hCA) isoforms I and II. AChE inhibition was in the range of 93.1 ± 33.7–467.5 ± 126.9 nM. The hCA I and II were effectively inhibited by these compounds, with Ki values in the range of 4.3 ± 1.1–9.1 ± 2.7 nM for hCA I and 4.2 ± 1.1–14.1 ± 4.4 nM for hCA II. On the other hand, acetazolamide clinically used as CA inhibitor showed Ki value of 13.9 ± 5.1 nM against hCA I and 18.1 ± 8.5 nM against hCA II. The antioxidant activity of the pyrimidine‐thiones derivatives ( A–K ) was investigated by using different in vitro antioxidant assays, including Cu2+ and Fe3+ reducing, 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH?) radical scavenging, and Fe2+ chelating activities. |
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| Keywords: | acetylcholinesterase antioxidant activity carbonic anhydrase enzyme inhibition pyrimidine‐thiones |
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