Novel tribenzylaminobenzolsulphonylimine based on their pyrazine and pyridazines: Synthesis, characterization, antidiabetic, anticancer, anticholinergic, and molecular docking studies.

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ID: 64015
2019
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Abstract
A new method of obtaining multifunctional pyrazoles by the reaction of 1,3-dipolar addition of tribenzylsulfonyliminochloride to polarophiles has been developed. This imine is obtained by reacting tribenzylamine with N-chlorobenzene sulfamide (chloramine-B). Regardless of the structure and composition of polarophiles, the cyclization reaction takes place in the presence of alkali in 6-8 h of boiling, which proves the activation of the methylene groups of tribenzylamine using the electron-withdrawing sulfonamide group. These novel derivatives were effective inhibitors of the α-glycosidase, butyrylcholinesterase (BChE), and acetylcholinesterase enzymes (AChE) with Ki values in the range of 0.45 ± 0.08-1.24 ± 0.27 µM for α-glycosidase, 6.04 ± 0.95-11.61 ± 2.84 µM for BChE, and 2.04 ± 0.24-4.23 ± 1.02 µM for AChE, respectively. The biological activities of the studied molecules against enzyme molecules were investigated by molecular docking calculations. The enzymes studied were AChE for ID 4M0E, BChE for ID 5NN0 BChE, and α-Glycosidase for ID 1XSI (α-Gly) respectively.
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mamedova2019novelbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Mamedova, Gulnar;Mahmudova, Adila;Mamedov, Sabir;Erden, Yavuz;Taslimi, Parham;Tüzün, Burak;Tas, Recep;Farzaliyev, Vagif;Sujayev, Afsun;Alwasel, Saleh H;Gulçin, İlhami;
Journal Bioorganic chemistry
Year 2019
DOI
S0045-2068(19)31386-0
URL
Keywords
molecular docking enzyme inhibition anticancer pyrazole cholinesterase sulfamide

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