80-09-1Relevant articles and documents
Sulfonylbis(acylhydrazones) as anticholinesterase inhibitors: Synthesis, in vitro biological evaluation and computational studies
Ahmad, Manzoor,Ahmad, Sajjad,Akbar, Nazia,Al-Harrasi, Ahmed,Ali, Akbar,Ali, Mumtaz,Ibrahim, Muhamad,Khan, Ajmal,Latif, Abdul,Saadiq, Mohammad,Siddique, Abu Bakar,farooq, Umar
, (2022/01/03)
This current research work is focused on the synthesis of sulfonyl-mediated hydrazones, its exploration as anticholinesterase inhibitors, in vitro biological evaluation, and computational studies. A series of 21 novel bis(acylhydrazones) (4a-u) have been synthesized in good to excellent yields using 4,4?-sulfonyldiphenol as the precursor. Characterization of the synthesized compounds was achieved via spectroscopic techniques i.e. UV, FT-IR, NMR (1H and 13C), and HRMS. In vitro anticholinesterase activity of these compounds was performed using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) as cholinesterase enzymes. Among all the compounds tested, compounds 4 g and 4 h were found to be the most significant AChE inhibitions with IC50 values of 101.4 and 102.7 μM as compared to the standard cholinesterase inhibitor i.e., galantamine (IC50 = 104.5 μM). Additionally, compound 4 g was also found to be an excellent inhibitor of BChE with an IC50 value of 136.0 μM as compared to the standard galantamine (IC50 = 156.8 μM). Molecular docking of the most active compounds 4 g and 4 h also supported their potential to interact with cholinesterase enzymes. Further affirmation on the intermolecular stability of the docked complexes was achieved by molecular dynamics simulation for 100 ns with mean deviations ~2 ?. Residue level fluctuations analysis also interpreted the good stability of compounds interacting pocket residues. Lastly, binding free energy analysis was performed that decipher the intermolecular interactions that are dominated by both van der Waals and electrostatic energies. In short, both theoretical and experimental studies unveiled the compounds as potent blockers of cholinesterase enzymes.
Selective synthesis of sulfoxides and sulfonesviacontrollable oxidation of sulfides withN-fluorobenzenesulfonimide
Cao, Zhong-Yan,Li, Xiaolong,Lu, Hao,Wang, Panpan,Wang, Shengqiang,Xu, Xiaobo,Yan, Leyu,Yang, A-Xiu
supporting information, p. 8691 - 8695 (2021/10/22)
A practical and mild method for the switchable synthesis of sulfoxides or sulfonesviaselective oxidation of sulfides using cheapN-fluorobenzenesulfonimide (NFSI) as the oxidant has been developed. These highly chemoselective transformations were simply achieved by varying the NFSI loading with H2O as the green solvent and oxygen source without any additives. The good functional group tolerance makes the strategy valuable.
Preparation process of low-cost and environment-friendly bisphenol S
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Paragraph 0034-0038; 0046-0050; 0058-0062, (2021/11/26)
The invention discloses a preparation process of bisphenol S with low cost and environmental protection. When the corrosion-resistant paint is sprayed into the interior of the reaction kettle, N atoms and O atoms of the reinforcing filler can interact with the metal ions to form a chelate. The acid resistance of the reaction kettle is higher, and the preparation cost is further reduced.