Design, Synthesis, and In Vitro Evaluation of the Leishmanicidal Activity of New Aromatic Symmetrical 1,4-Disubstituted 1,2,3-Bistriazoles.

ABSTRACT: A second generation of symmetrical 1,4-disubstituted 1,2,3-triazoles containing aromatic moieties was designed and synthesized from 2-hydroxy-1,3-bisazido-propane and terminal alkynes by copper-(I)-catalyzed alkyne-azide cycloaddition (CuAAC) as potential inhibitors of protein CYP51. The symmetrical bistriazoles (SBs) were obtained in moderate to excellent yields (49 to 95%). All synthetic nonsymmetric triazoles and the symmetric bistriazole derivatives were in vitro screened for the extracellular promastigote forms of . From this investigation, it emerged that symmetric bistriazole 12c (IC₅₀ = 19.24 μM) showed the highest potency against the flagellate form of the parasite followed by compounds 12b (IC₅₀ = 34.46 μM), 10 (IC₅₀ = 44.13 μM), and 4 (IC_50<

SUBMITTER: Victor MM 

PROVIDER: S-EPMC12242654 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature