Title : Novel tribenzylaminobenzolsulphonylimine based on their pyrazine and pyridazines: Synthesis, characterization, antidiabetic, anticancer, anticholinergic, and molecular docking studies - Mamedova_2019_Bioorg.Chem_93_103313 |
Author(s) : Mamedova G , Mahmudova A , Mamedov S , Erden Y , Taslimi P , Tuzun B , Tas R , Farzaliyev V , Sujayev A , Alwasel SH , Gulcin I |
Ref : Bioorg Chem , 93 :103313 , 2019 |
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 6-8h 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 alpha-glycosidase, butyrylcholinesterase (BChE), and acetylcholinesterase enzymes (AChE) with Ki values in the range of 0.45+/-0.08-1.24+/-0.27microM for alpha-glycosidase, 6.04+/-0.95-11.61+/-2.84microM for BChE, and 2.04+/-0.24-4.23+/-1.02microM 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 alpha-Glycosidase for ID 1XSI (alpha-Gly) respectively. |
PubMedSearch : Mamedova_2019_Bioorg.Chem_93_103313 |
PubMedID: 31586711 |
Mamedova G, Mahmudova A, Mamedov S, Erden Y, Taslimi P, Tuzun B, Tas R, Farzaliyev V, Sujayev A, Alwasel SH, Gulcin I (2019)
Novel tribenzylaminobenzolsulphonylimine based on their pyrazine and pyridazines: Synthesis, characterization, antidiabetic, anticancer, anticholinergic, and molecular docking studies
Bioorg Chem
93 :103313
Mamedova G, Mahmudova A, Mamedov S, Erden Y, Taslimi P, Tuzun B, Tas R, Farzaliyev V, Sujayev A, Alwasel SH, Gulcin I (2019)
Bioorg Chem
93 :103313