126799-96-0Relevant academic research and scientific papers
Synthesis, inhibition properties against xanthine oxidase and molecular docking studies of dimethyl N-benzyl-1H-1,2,3-triazole-4,5-dicarboxylate and (N-benzyl-1H-1,2,3-triazole-4,5-diyl)dimethanol derivatives
Yagiz, Güler,Noma, Samir Abbas Ali,Altundas, Aliye,Al-khafaji, Khattab,Taskin-Tok, Tugba,Ates, Burhan
, (2021/01/28)
This study focused on synthesis various dimethyl N-benzyl-1H-1,2,3-triazole-4,5-dicarboxylate and (N-benzyl-1H-1,2,3-triazole-4,5-diyl)dimethanol derivatives under the conditions of green chemistry without the use of solvent and catalysts. Their inhibition properties were also investigated on xanthine oxidase (XO) activity. All dimethanol and dicarboxylate derivatives exhibited significant inhibition activities with IC50 values ranging from 0.71 to 2.25 μM. Especially, (1-(3-bromobenzyl)-1H-1,2,3-triazole-4,5-diyl)dimethanol (5c) and dimethyl 1-(4-chlorobenzyl)-1H-1,2,3-triazole-4,5-dicarboxylate (6 g) compounds were found to be the most promising derivatives on the XO enzyme inhibition with IC50 values 0.71 and 0.73 μM, respectively. Moreover, the double docking procedure was to evaluate compound modes of inhibition and their interactions with the protein (XO) at atomic level. Surprisingly, the docking results showed a good correlation with IC50 [correlation coefficient (R2 = 0.7455)]. Also, the docking results exhibited that the 5c, 6f and 6 g have lowest docking scores ?4.790, ?4.755, and ?4.730, respectively. These data were in agreement with the IC50 values. These results give promising beginning stages to assist in the improvement of novel and powerful inhibitor against XO.
1,2,3-triazolo [4,5-d] pyridazines-V. Preparation and adenosine receptor binding of new 4-amino derivatives
Biagi,Giorgi,Livi,Manera,Scartoni,Lucacchini,Senatore
, p. 601 - 608 (2007/10/03)
This paper reports the continuation of studies on the 4-aminosubstituted 1,2,3-triazolo [4,5-d] pyridazine derivatives which had shown binding affinity towards A1-adenosine receptors. 1-Benzyl derivatives bearing new amines and new 1-(substituted benzyl) derivatives were prepared and tested. The biological results showed that some compounds possessed high affinity (~30-70 nM) and good selectivity toward the A1-adenosine receptors. Further information about structure-biological activity relationships was acquired.
Dipolar Cycloaddition Reactions of Organic Azides with some Acetylenic Compounds
Abu-Orabi, Sultan T.,Atfah, M. Adnan,Jibril, Ibrahim,Mari'i, Fakhri M.,Ali, Amer Al-Sheikh
, p. 1461 - 1468 (2007/10/02)
Phenyl azide 1 and several substituted benzyl azides 2a-o underwent 1,3-dipolar cycloaddition reactions with dimethyl acrtylenedicarboxylate 3, phenylacetylene 4 and ethyl propiolate 5 to afford the triazoles 6-13.The reactions of these azides with ethyl
Aralkyltriazole compounds
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, (2008/06/13)
1-phenyl-lower alkyl-1H-1,2,3-triazole compounds of the formula STR1 in which Ph represents phenyl substituted by up to and including 3 substituents selected from lower alkyl, halogen and trifluoromethyl, alk represents lower alkylidene, and wherein either R1 represents hydrogen, lower alkyl, lower alkoxy, amino, N-lower alkylamino, N,N-di-lower alkylamino, N-lower alkanoylamino, carbamoyl, N-lower alkanoylcarbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl and R2 represents carbamoyl, N-lower alkanoylcarbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl or R1 represents carbamoyl, N-lower alkanoylcarbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl and R2 represents hydrogen or lower alkyl, have anti-convulsive properties and can be used as medicaments.
