3718-22-7Relevant articles and documents
Synthesis, in-vitro and in-silico studies of triazinoindole bearing bis-Schiff base as β-glucuronidase inhibitors
Ahmad, Shakeel,Aziz, Aamir,Khan, Fahad,Rahim, Fazal,Sarfraz, Maliha,Taha, Muhammad,Ullah, Hayat,Wadood, Abdul
, (2021/07/16)
Triazinoindole bearing bis-Schiff base analogs (1–20) were synthesized by triazinoindole-thione ring formation, triazinoindole-thiol-phenylethanone, followed by triazinoindole bis-Schiff base formation. Synthesized analogs showed β-glucuronidase potential with IC50 value ranging between 2.60 ± 0.10 to 55.40 ± 1.60 μM as compared to standard D-saccharic acid 1,4-lactone (IC50 = 48.10 ± 1.2 μM). Analog 20 was the most potent one with IC50 value 2.60 ± 0.10 μM. Analogs 17, 4 showed IC50 values 5.20 ± 0.20 and 5.70 ± 0.20 μM respectively and withstand 2nd and 3rd ranked scaffolds among the synthesized analogs. All other sixteen analogs showed many-fold better potency with IC50 values ranging from 7.9 ± 0.2 to 48.1 ± 1.2 μM. The structure-activity relationship was established and confirmed of binding interactions through molecular docking studies.
Metal schiff base complexes of tridentate antipyrine based ligand: Synthesis, spectral characterisation, image analysis and biological studies
Dhanaraj, C. Justin,Jebapriya, M.
, (2020/07/03)
Novel tridentate antipyrine based ligand (L) were synthesized and characterized employing analytical, spectral and image processing techniques. The Co(II), Ni(II), Cu(II) and Zn(II) complexes of newly synthesized L is characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, FTIR, UV–visible, 1H NMR, 13C NMR, and mass spectrometry. Octahedral geometry is given to Co(II), Ni(II) and Zn(II) complexes, whereas Cu(II) complex preferred distorted octahedral geometry. The ligand to metal ratio was identified to be 1:1. Thermal stability of the new integrated compounds were inspected by thermogravimetric analysis. Porosity of the complexes is analysed by image processing. The electrochemical deportment of the Schiff base metal complexes was assessed using cyclic voltammetry. In vitro antimicrobial, DNA cleavage and SOD efficacy of the present compounds were determined. The in vitro anticancer potency of the metal complexes were also evaluated against Liver Bilobular cancerous cells (LBir2754).
Efficient Multigram Approach to Acetylenes and CF3-ynones Starting from Dichloroalkenes Prepared by Catalytic Olefination Reaction (COR)
Muzalevskiy, Vasiliy M.,Sizova, Zoia A.,Diusenov, Arstan I.,Shastin, Alexey V.,Nenajdenko, Valentine G.
supporting information, p. 4161 - 4166 (2020/07/13)
A novel approach to terminal acetylenes based on catalytic olefination reaction COR of arylaldehydes to form dichloroalkenes followed by treatment with nBuLi was elaborated. This method is atom economical and displays high yields and effectivity. The corresponding alkynes can be prepared in up to 97 % yield. One pot procedure towards CF3-ynones was elaborated to provide these products in up to 87 % yield starting from dichloroalkenes.