Discovery of novel 1,2,4-triazole tethered β-hydroxy sulfides as bacterial tyrosinase inhibitors: synthesis and biophysical evaluation through in vitro and in silico approaches.

ABSTRACT: In this study, a series of 1,2,4-triazole-tethered β-hydroxy sulfide scaffolds 11a-h was synthesized in good to remarkable yields (69-90%) through the thiolysis of oxiranes by the thiols in aqueous basic catalytic conditions. The synthesized 1,2,4-triazole-tethered β-hydroxy sulfides were screened against bacterial tyrosinase enzyme, and Gram-positive and Gram-negative bacterial cultures i.e., (S. aureus) Staphylococcus aureus & (E. coli) Escherichia coli. Among the synthesized derivatives, the molecules 11a (IC₅₀ = 7.67 ± 1.00 μM), 11c (IC₅₀ = 4.52 ± 0.09 μM), 11d (IC₅₀ = 6.60 ± 1.25 μM), and 11f (IC₅₀ = 5.93 ± 0.50 μM) displayed the better tyrosinase inhibitory activity in comparison to reference drugs ascorbi

SUBMITTER: Saeed S 

PROVIDER: S-EPMC11089527 | biostudies-literature | 2024 May

REPOSITORIES: biostudies-literature