7265-27-2Relevant academic research and scientific papers
Synthesis, biological evaluation, theoretical investigations, docking study and ADME parameters of some 1,4-bisphenylhydrazone derivatives as potent antioxidant agents and acetylcholinesterase inhibitors
Amine Khodja, Imene,Boulebd, Houssem
, p. 279 - 290 (2021)
Abstract: Five 1,4-bisphenylhydrazone derivatives (1–5) were successfully synthesized and evaluated for their antioxidant and acetylcholinesterase inhibitory activities. The antioxidant activity has been carried out using DPPH, ABTS, CUPRAC and superoxide radical scavenging methods. All the compounds showed a very good antioxidant activity compared to that of the standards used. Compound 1 was found to be the best antioxidant agent with IC50 values lower or comparable to that of the standards. The acetylcholinesterase inhibitory activity has been evaluated using a modified Ellman’s assay. The obtained results indicate that compound 2 is the best acetylcholinesterase inhibitor with a low IC50 value comparable to that of the galantamine. In addition, DFT calculations have been performed to determine in which mechanism the synthesized hydrazones follow to scavenge free radicals. Molecular docking study was performed for compound 2, and its interaction modes with the enzyme acetylcholinesterase were determined. As a result, a strong interaction between this compound and the active site of AChE enzyme was revealed. Finally, ADME properties of the synthesized compounds were also studied and showed good drug-like properties. Graphic abstract: [Figure not available: see fulltext.]
Synthesis of Symmetric Binuclear 5,6-Dihydro-1,2,4,5-tetrazinium Perchlorates
Asfandeev, A. Yu.,Burtasov, A. A.,Idris, T. D.,Kostryukov, S. G.,Kozlov, A. Sh.,Krasnov, D. A.,Petrov, P. S.,Tezikova, V. S.
, p. 614 - 620 (2021/06/02)
Abstract: A series of 3,3′-(1,4-phenylene)bis(1-4-R-phenyl)-5-phenyl-5,6-dihydro-1,2,4,5-tetrazinium) perchlorates (R = H, Me, Cl, OMe, CN, NO2) were obtained as a result of a three-stage synthesis from terephthalic aldehyde. The synthesis of tetrazinium salts was carried out by reaction of the corresponding formazans with formalin in the presence of perchloric acid in dioxane. Formazans and tetrazinium perchlorates were isolated in individual state and characterized by elemental analysis, IR, UV, 1H, and 13C NMR spectroscopy data. The process of electrochemical reduction of tetrazinium perchlorates was studied using the method of cyclic voltammetry (CV). It has been shown that these compounds are perspective precursors of symmetric biradical systems based on verdazyl radicals.
Organofluorine Hydrazone Derivatives as Multifunctional Anti-Alzheimer's Agents with CK2 Inhibitory and Antioxidant Features
Baier, Andrea,Kokel, Anne,Horton, William,Gizińska, Ewa,Pandey, Garima,Szyszka, Ryszard,T?r?k, Béla,T?r?k, Marianna
, p. 1927 - 1932 (2021/04/19)
A set of novel hydrazone derivatives were synthesized and analyzed for their biological activities. The compounds were tested for their inhibitory effect on the phosphorylating activity of the protein kinase CK2, and their antioxidant activity was also de
Design, synthesis, biological and in silico evaluation of phenylene (bis) hydrazone derivatives against osteosarcoma cancer
Govindaiah, Pilli,Kumar, Rakesh,Guttula, Praveen Kumar,Gupta, Mukesh Kumar,Jaya Prakash
, p. 2638 - 2645 (2021/01/05)
Three sets of differentphenylene-bis(hydrazone) derivatives namely,Gc, Gd and Ge,were designed, synthesized and evaluated for their molecular properties andin vitro anticancer activity against human osteosarcoma MG-63 cells. All compounds showed potent an
