123-00-2Relevant articles and documents
New asymmetrical morpholinium- and 1,1-dioxidothiomorpholinium-based dicationic ionic liquid: structure, thermophysical and electrochemical properties of propylene carbonate solutions
Arkhipova, Ekaterina A.,Ivanov, Anton S.,Levin, Mikhail M.,Maslakov, Konstantin I.,Kupreenko, Stepan Yu.,Lyssenko, Konstantin A.,Savilov, Serguei V.
, (2021/08/09)
A new asymmetrical 1,1-dioxidothiomorpholinium- and morpholinium-based dicationic ionic liquid (4-ethyl-4-[3-(4-ethyl-1,1-dioxidothiomorpholin-4-ium-4-yl)propyl]morpholin-4-ium tetrafluoroborate (EtDTMC3EtM·2BF4)) was synthesized in four stages and characterized by 1H, 13C, 1H,1H–COSY NMR, single X-ray diffraction, XPS spectroscopy and simultaneous thermal analysis. Electrical conductivities of several EtDTMC3EtM·2BF4 solutions in propylene carbonate (PC) were measured in the 298 – 368 K temperature range and analyzed using the Arrhenius, Litovitz, and Vogel–Fulcher–Tammann (VFT) equations.
Highly Selective Butyrylcholinesterase Inhibitors with Tunable Duration of Action by Chemical Modification of Transferable Carbamate Units Exhibit Pronounced Neuroprotective Effect in an Alzheimer's Disease Mouse Model
Hoffmann, Matthias,Stiller, Carina,Endres, Erik,Scheiner, Matthias,Gunesch, Sandra,Sotriffer, Christoph,Maurice, Tangui,Decker, Michael
, p. 9116 - 9140 (2019/11/03)
In this study, the carbamate structure of pseudo-irreversible butyrylcholinesterase (BChE) inhibitors was optimized with regard to a longer binding to the enzyme. A set of compounds bearing different heterocycles (e.g., morpholine, tetrahydroisoquinoline, benzimidazole, piperidine) and alkylene spacers (2 to 10 methylene groups between carbamate and heterocycle) in the carbamate residue was synthesized and characterized in vitro for their binding affinity, binding kinetics, and carbamate hydrolysis. These novel BChE inhibitors are highly selective for hBChE over human acetycholinesterase (hAChE), yielding short-, medium-, and long-acting nanomolar hBChE inhibitors (with a half-life of the carbamoylated enzyme ranging from 1 to 28 h). The inhibitors show neuroprotective properties in a murine hippocampal cell line and a pharmacological mouse model of Alzheimer's disease (AD), suggesting a significant benefit of BChE inhibition for a disease-modifying treatment of AD.
INHIBITORS OF BACTERIAL GLYCOSYL TRANSFERASES
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Paragraph 00366; 00437-00438, (2016/12/22)
Described herein are compounds of Formula (I'), Formula (IA), Formulae (I)-(VII), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrug sthereof. The invention also provides pharmaceutical compositions of the compounds for human and veterinary use. Compounds of the present invention are useful for inhibiting bacterial growth and therefore are useful in treating and/or preventing bacterial infections. Methods of using the compounds for treating and/or preventing a bacterial infection in a subject are also described.