Gulcin_2020_Bioorg.Chem_103_104171

Reference

Title : Synthesis of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds - Determination of their carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase and alpha-glycosidase inhibition properties - Gulcin_2020_Bioorg.Chem_103_104171
Author(s) : Gulcin I , Trofimov B , Kaya R , Taslimi P , Sobenina L , Schmidt E , Petrova O , Malysheva S , Gusarova N , Farzaliyev V , Sujayev A , Alwasel S , Supuran CT
Ref : Bioorg Chem , 103 :104171 , 2020
Abstract :

Sulfur-containing pyrroles (1-3), tris(2-pyridyl)phosphine(selenide) sulfide (4-5) and 4-benzyl-6-(thiophen-2-yl)pyrimidin-2-amine (6) were synthesized and characterized by elemental analysis, IR and NMR spectra. In this study, the synthesized compounds of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds (1-6) were evaluated against the human erythrocyte carbonic anhydrase I, and II isoenzymes, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and alpha-glycosidase enzymes. The synthesized heterocyclic compounds showed IC(50) values in range of 33.32-60.79 nM against hCA I, and 37.05-66.64 nM against hCA II closely associated with various physiological and pathological processes. On the other hand, IC(50) values were found in range of 13.13-22.21 nM against AChE, 0.54-31.22 nM against BChE, and 13.51-26.55 nM against alpha-glycosidase as a hydrolytic enzyme. As a result, nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds (1-6) demonstrated potent inhibition profiles against indicated metabolic enzymes. Therefore, we believe that these results may contribute to the development of new drugs particularly in the treatment of some global disorders including glaucoma, Alzheimer's disease and diabetes.

PubMedSearch : Gulcin_2020_Bioorg.Chem_103_104171
PubMedID: 32891857

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Gulcin I, Trofimov B, Kaya R, Taslimi P, Sobenina L, Schmidt E, Petrova O, Malysheva S, Gusarova N, Farzaliyev V, Sujayev A, Alwasel S, Supuran CT (2020)
Synthesis of nitrogen, phosphorus, selenium and sulfur-containing heterocyclic compounds - Determination of their carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase and alpha-glycosidase inhibition properties
Bioorg Chem 103 :104171

Gulcin I, Trofimov B, Kaya R, Taslimi P, Sobenina L, Schmidt E, Petrova O, Malysheva S, Gusarova N, Farzaliyev V, Sujayev A, Alwasel S, Supuran CT (2020)
Bioorg Chem 103 :104171