3115-21-7Relevant articles and documents
4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
Secci, Daniela,Carradori, Simone,Petzer, Anél,Guglielmi, Paolo,D’Ascenzio, Melissa,Chimenti, Paola,Bagetta, Donatella,Alcaro, Stefano,Zengin, Gokhan,Petzer, Jacobus P.,Ortuso, Francesco
, p. 597 - 612 (2019/02/14)
A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure–activity relationships. The results of the biological testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a phenyl ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from molecular modelling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.
Catalytic synthesis of organic cyclic carbonate through CO2 fixation and production of β-amino alcohol via ring opening of epoxides under green condition by polystyrene embedded Al(III) catalyst
Biswas, Surajit,Roy, Dipanwita,Ghosh, Swarbhanu,Islam, Sk Manirul
, (2019/08/06)
Development of low cost, eco-friendly heterogeneous catalyst for the production of value added organic compounds has been drawn a considerable attention to the synthetic chemists in recent era. Keeping the above idea in our mind, we have design and synthesized a polymer anchored Al(III) composite from modified Merrifield resin. The composite was characterized properly by FT-IR spectra, SEM, EDAX, elemental analysis, ICP-AES and PXRD studies. The low cost material is very efficient heterogeneous catalyst for the production of fine organic chemicals such as organic cyclic carbonates and 2-amino alcohols under green and mild reaction conditions. Organic cyclic carbonates were synthesized through the insertion of carbon dioxide into epoxides at room temperature under solvent free condition. The developed protocol of catalytic synthesis of cyclic carbonates is sustainable, eco-friendly and cost-effective. Moreover atmospheric carbon dioxide is utilized here. Besides, the catalyst is very much efficient to produce 2-amino alcohol from ring opening of epoxides by nucleophilic attack of amine under solvent free condition and at room temperature. This polymer anchored Al(III) can be recovered and reused easily. The catalyst preserved its catalytic intensity even after use of eight successive catalytic cycles.
Synthesis and use of dioxime ligands for treatment of leukemia and colon cancer cells
Babahan, Ilknur,?zmen, Ali,Aslan, Kadir
, (2017/09/30)
Two new vicinal dioxime ligands containing thiosemicarbazone units (L1H2 and L2H2) were synthesized and characterized using 1H NMR, 13C NMR, heteronuclear multiple quantum correlation, mass, infrared and UV–visible spectroscopies, elemental analysis and magnetic susceptibility measurements. In addition, homotrinuclear nickel(II), copper(II) and cobalt(II) complexes with a metal-to-ligand ratio of 3:2 for L1H2 and L2H2 were prepared. Synthesis of nickel(II) complex containing a BF2 + bridge was carried out using a precursor hydrogen-bridged nickel(II) complex via the template effect. All metal–ligand complexes were tested against two human cancer cell lines (HL-60 and HT-29) for their antiproliferative and apoptotic activities. The results showed that [Co(L2H)2(H2O)2] and [Ni(L2H)2] exhibited the strongest antiproliferative activity with IpC50 values ranging between 5 and 10?μM, while [Co(L2H)2(H2O)2] and [Ni(L2H)2] both induced necrosis of HT-29 cells and 60 and 65% apoptosis in HL-60 cells, respectively.