N-Substituted pyrimidinethione and acetophenone derivatives as a new therapeutic approach in diabetes
Corresponding Author
Parham Taslimi
Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
Correspondence Parham Taslimi, Department of Biotechnology, Faculty of Science, Bartin University, 74100 Bartin, Turkey.
Email: [email protected]; [email protected]
Search for more papers by this authorAfsun Sujayev
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorMuhammet Karaman
Department of Molecular Biology and Genetics, Faculty of Arts and Science, Kilis 7 Aralik University, Kilis, Turkey
Search for more papers by this authorGunel Maharramova
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorNastaran Sadeghian
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorSabiya Osmanova
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorSabira Sardarova
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorNargiz Majdi
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorHandan U. Ozel
Department of Environmental Engineering, Faculty of Engineering, Bartin University, Bartin, Turkey
Search for more papers by this authorİlhami Gulcin
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorCorresponding Author
Parham Taslimi
Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
Correspondence Parham Taslimi, Department of Biotechnology, Faculty of Science, Bartin University, 74100 Bartin, Turkey.
Email: [email protected]; [email protected]
Search for more papers by this authorAfsun Sujayev
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorMuhammet Karaman
Department of Molecular Biology and Genetics, Faculty of Arts and Science, Kilis 7 Aralik University, Kilis, Turkey
Search for more papers by this authorGunel Maharramova
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorNastaran Sadeghian
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorSabiya Osmanova
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorSabira Sardarova
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorNargiz Majdi
Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, Azerbaijan
Search for more papers by this authorHandan U. Ozel
Department of Environmental Engineering, Faculty of Engineering, Bartin University, Bartin, Turkey
Search for more papers by this authorİlhami Gulcin
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorAbstract
In this study, compounds with 4-hydroxybutyl, 4-phenyl, 5-carboxylate, and pyrimidine moieties were determined as α-glycosidase inhibitors. N-Substituted pyrimidinethione and acetophenone derivatives (A1–A5, B1–B11, and C1–C11) were good inhibitors of the α-glycosidase enzyme, with Ki values in the range of 104.27 ± 15.75 to 1,004.25 ± 100.43 nM. Among them, compound B7 was recorded as the best inhibitor, with a Ki of 104.27 ± 15.75 nM against α-glycosidase. In silico studies were carried out to clarify the binding affinity and interaction mode of the compounds with the best inhibition score against α-glycosidase from Saccharomyces cerevisiae. Compounds B7 (S) and B11 (R) exhibited a good binding affinity with docking scores of −8.608 and 8.582 kcal/mol, respectively. The docking results also showed that the 4-hydroxybutyl and pyrimidinethione moieties play a key role in S. cerevisiae and human α-glycosidase inhibition.
CONFLICTS OF INTEREST
The authors declare that there are no conflicts of interests.
Supporting Information
| Filename | Description |
|---|---|
| ardp202000075-sup-0001-ArchPharm_SupplMat_InChI_2020_17_05_2020.doc213 KB | Supporting information |
| ardp202000075-sup-0002-Supplementary_mod.docx3.1 MB | Supporting information |
Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
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