Sepehri, Nima; Khoshneviszadeh, Mehdi; Farid, Sara Moghadam; Moayedi, Seyedeh Sara; Asgari, Mohammad Sadegh; Moazzam, Ali; Hosseini, Samanesadat; Adibi, Hossein; Larijani, Bagher; Pirhadi, Somayeh; Attarroshan, Mahshid; Sakhteman, AmirHossein; Kabiri, Maryam; Hamedifar, Haleh; Iraji, Aida; Mahdavi, Mohammad published the artcile< Design, synthesis, biological evaluation, and molecular docking study of thioxo-2,3-dihydroquinazolinone derivative as tyrosinase inhibitors>, Related Products of 3731-53-1, the main research area is thioxo dihydroquinazolinone preparation antioxidant docking tyrosinase inhibitor.
In this study, a series of thioxo-dihydroquinazolinone compounds I (R1 = i-Pr, Ph, pyridin-3-ylmethyl, cyclopentyl, etc.) were designed and synthesized as tyrosinase inhibitors. Among the investigated compounds, I (R1 = i-Pr (III)) demonstrated the best inhibitory activity with an IC50 value of 15.48μM compared to kojic acid as a pos. control with IC50 value of 9.30μM. In kinetic evaluation against tyrosinase, (III) depicted a mixed inhibition pattern. Addnl., antioxidant evaluations exhibited moderate to weak potency in 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The detailed interactions and binding mode toward tyrosinase of the most potent derivative were explicated by mol. docking study. Moreover, the computer-aided drug-likeness and pharmacokinetic studies were also carried out.
Journal of Molecular Structure published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Related Products of 3731-53-1.