Natural L-carvone was utilized as a starting material for an efficient synthesis of some terpenyl-derived 1,2,3-triazoles. Chlorination of carvone, followed by nucleophilic substitution with sodium azide resulted in the preparation of 10-azidocarvone. Subsequent CuAAC click reaction with propargylated derivatives provided an efficient synthetic route to a set of terpenyl-derived conjugates with increased solubility in water. All investigated compounds exhibit high antioxidant activity, which is comparable with that of vitamin C. It was also found that serum albumin and the terpenyl-1,2,3-triazoles hybrids spontaneously undergo reversible binding driven by hydrophobic interactions, suggesting that serum albumin can transport the target triazoles.

A method for the preparation of methyl esters of β-1,2,4triazole-substituted alanines by condensation of methyl acrylate with 3,4-disubstituted-5-mercapto-1,2,4-triazoles has been developed. The optimal conditions for the process of hydrazinolysis of N-allyl derivatives of the obtained products were established. It is shown that to prevent the reduction of the allyl group, it is reasonable to carry out the process of hydrazinolysis in the presence of sodium sulfite. Based on hydrazides of β-1,2,4-triazole-substituted alanines, biheterocyclic compounds of a new structure -1,2,4-triazole-and 1,3,4oxadiazole-1,2,4-triazoles were synthesized.ChemistrySelect 2018, 3, 9981 -9985

The synthesis of new derivatives of 3‐(3‐arylprop‐2‐ynyl)dihydrofuran‐2(3H)‐ones by Sonogashira reactions and their screening as potent and selective inhibitors of b‐TNAP is reported. Although a few derivatives exhibited non‐selective inhibition of c‐IAP, most of the derivatives were found to be potent and selective inhibitors of b‐TNAP. The selective and potent inhibitors of b‐TNAP might be useful for the treatment of vascular calcification. Among the derivatives studied, one compound was identified as the most potent inhibitor of b‐TNAP with a high inhibitory value, exhibiting a 6 fold more selective activity towards b‐TNAP as compared to c‐IAP. The higher inhibitory activity of this compound towards b‐TNAP is caused by the presence of two furan rings. Similarly, another derivative, having a furan ring, exhibited a lower inhibitory potential towards b‐TNAP, but this compound was found to be the most potent inhibitor of c‐IAP. Furthermore, molecular docking studies of these potent compounds were carried out to see the possible binding modes of potent inhibitors inside the active pocket of respective enzyme.

1,2,3-Triazoles have attracted the interest of researchers due to their wide range of biological activities which include antitumor, anti-leishmanial, bioluminescent and fungicidal activities This paper describes the synthesis of novel triazole hybrids containing biologically active fragments through cycloaddition (click) reactions, with the aim of increasing the diversity of known and active 1,2,3-triazole derivatives. All new compounds have been characterized by physicochemical methods.

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