Design and Synthesis of New 5-aryl-4-Arylethynyl-1H-1,2,3-triazoles with Valuable Photophysical and Biological Properties [PDF]
Cu-catalyzed 1,3-dipolar cycloaddition of methyl 2-azidoacetate to iodobuta-1,3-diynes and subsequent Suzuki-Miyaura cross-coupling were used to synthesize new triazoles derivatives: 5-aryl-4-arylethynyl-1H-1,2,3-triazoles. Investigation of their optical
Mariia M. Efremova +4 more
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In vitro combination effects and mechanisms of Revaprazan with Triazole antifungal drugs on Aspergillus [PDF]
Potassium-competitive acid blockers (P-CABs), such as revaprazan (REV), act by competitively inhibiting potassium (K+) binding on the proton pump (H+/K+-ATPase) and are reversible K+ antagonists.
Wenxu Cheng +6 more
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Azide–alkyne cycloaddition (click) reaction in biomass-derived solvent CyreneTM under one-pot conditions [PDF]
It was demonstrated that CyreneTM, as a biomass-originated polar aprotic solvent, could be utilized as an alternative reaction medium for one-pot copper(I)-catalyzed azide–alkyne cycloaddition (click or CuAAC) reactions, for the synthesis of various 1,2 ...
Zoltán Medgyesi, László T. Mika
doaj +2 more sources
Purpose: Torsade de pointes (TdP)/QT prolongation is a fatal adverse event (AE) when using antifungal triazoles. We aimed to compare the AE signals of TdP/QT prolongation and onset time among different drugs of this kind comprehensively.
Zicheng Yu, Xiaolan Liao
doaj +1 more source
Aim. To analyze and summarize the synthetic potential of 1,2,3-triazole-4(5)-amines as efficient building blocks in the synthesis of triazolo-annulated pyridine, azine and azepine systems. Results and discussion.
Natalia O. Syrota +3 more
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To select a molecule that could become a promising pharmacological agent, chemists use already-known heterocyclic bases by adding pharmacologically active groups. One such heterocyclic system is 1,2,4-triazole base, on the basis of which a huge number of
A. A. Safonov, O. I. Panasenko
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Determination of the pKa value of some 1,2,4-triazol derivatives in forty seven different solvents using semi-empirical quantum methods (PM7, PM6, PM6-DH2, RM1, PM3, AM1, and MNDO) by MOPAC computer program [PDF]
In this study, we calculated the enthalpy (?H, kcal/mol), entropy (?S, cal/K.mol) and free energy (?G, kcal/mol) thermodynamic values of each molecule for forty-seven different solvent media according to semi-empirical quantum methods (PM7, PM6, PM6-DH2,
Erdoğan, Naciye +2 more
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Discovery of a new class of triazole based inhibitors of acetyl transferase KAT2A
We have recently developed a new synthetic methodology that provided both N-aryl-5-hydroxytriazoles and N-pyridine-4-alkyl triazoles. A selection of these products was carried through virtual screening towards targets that are contemporary and validated ...
Roberta Pacifico +9 more
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A series of neat 4-(2-alkenyl) substituted 5-methyl-3-phenyl-4H-1,2,4-triazoles were thermolyzed at 320 oC producing a rearrangement products, of which the regioisomeric 1- and 2-substituted triazoles were the main products.
Per H.J. Carlsen +2 more
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Iterative in Situ Click Chemistry Assembles a Branched Capture Agent and Allosteric Inhibitor for Akt1 [PDF]
We describe the use of iterative in situ click chemistry to design an Akt-specific branched peptide triligand that is a drop-in replacement for monoclonal antibodies in multiple biochemical assays.
Agnew, Heather D. +12 more
core +2 more sources

