Functionalized 1,2,3-triazolium salts as potential agents against visceral leishmaniasis

Research Advances on the Bioactivity of 1,2,3-Triazolium Salts

“…In addition, compound 38 exhibited a low cytotoxic effect on macrophages, with a CC 50 value of 47.92 µM ( Figure 17 ). In the inhibition test against intracellular amastigotes, compound 38 also showed good activity (IC 50 = 7.92 µM), with an SI of 6.05 [ 12 ].…”

“…Compounds 36 , 37 , and 38 bearing 10-carbon side chains at the N-1 position and a methyl group at the N-3 position exhibit good antileishmanial activities [ 12 , 43 , 44 ]. The long carbon chain at the N-1 position of these compounds is beneficial to their antileishmanial activities.…”

“…The long carbon chain at the N-1 position of these compounds is beneficial to their antileishmanial activities. The analogs of compound 38 containing 12, 14, or 16 carbon atoms in the alkyl side chain exhibit better antileishmanial activities, but the long carbon chain also leads to strong toxicity against macrophages [ 12 ]. Furthermore, those 1,2,3-triazolium salts bearing a propyl group on the N-3 position exhibit a strong toxic effect on macrophages, regardless of the length of the side chain [ 12 ].…”

“…The analogs of compound 38 containing 12, 14, or 16 carbon atoms in the alkyl side chain exhibit better antileishmanial activities, but the long carbon chain also leads to strong toxicity against macrophages [ 12 ]. Furthermore, those 1,2,3-triazolium salts bearing a propyl group on the N-3 position exhibit a strong toxic effect on macrophages, regardless of the length of the side chain [ 12 ]. It is worth noting that the 1,2,3-triazolium group is crucial for enhancing the antileishmanial activities of the compounds, since compounds 37 and 38 exhibit higher antileishmanial activities than their parent triazole [ 12 , 44 ].…”

“…The 1,2,3-triazolium unit is a significant bioactive group, which has attracted much attention in recent years [ 3 , 4 ]. Studies have shown that the triazolium transformated from triazole have good bioactivities [ 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 ]. Molecules containing 1,2,3-triazolium units have been proven to exhibit a variety of biological activities, including antibacterial [ 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 ], antifungal [ 5 , 6 , 7 , 8 , 9 , 35 ], anticancer [ 10 , 11 , 36 , 37 , 38 , 39 , 40 , 41 , 42 ], and antileishmanial [ 12 , 43 , 44 , 45 , 46 ] properties.…”