5-[2-(N,N-diethylamino)ethoxy]-4,7-dimethylcoumarin (1) and 6-acetyl-5-[2-(N,N-diethylamino)ethoxy]-4,7-dimethylcoumarin (2) were synthesized in a traditional way and microwave-assisted synthesis. Crystals of 2 in form of hydrochloride salt (3) were investigated using single crystal X-ray diffra...
2-Diethylaminoethyl p-aminobenzoate is unstable at elevated temperatures and evolves carbon dioxide, 2-diethylaminoethanol, and N,N-diethyl-N′-phenylethylenediamine. The pharmacological properties of the diamine correlate with some of the actions of systemic procaine.
The rates of the base-catalyzed proton exchange and inversion (epimerization) at chiral nitrogen centers of [Co(acac)2(Ph-en)]+ (acac=2,4-pentanedionate ion; Ph-en=N-phenylethylenediamine) and [Co(acac)2(Me-en)]+ (Me-en=N-methylethylenediamine) in aqueous solutions have been measured at 34.0 °C...
The [Co(acac)2(N-phenylethylenediamine)]+ (acac= 2,4-pentanedionate ion)and[Co(acac)2(N,N′-diphenylethylenediamine)]+ complexes were separated into two and three racemic pairs of the diastereomers, respectively, by means of column chromatography and the diastereomers were resolved by the chemic...
A new amine bis(phenol) ligand (HLPEA), was synthesized and characterized by IR, 1H NMR spectroscopic techniques and elemental analyses. The mononuclear iron(III) complex (FeLPEA) of this ligand has been prepared and characterized by IR and UV–Vis spectroscopic techniques, ESI-MS, elemental ana...
Neovascularization may contribute to functional recovery after neural injury. Combination treatment of stroke with a nitric oxide donor, (Z)-1-[N-(2-aminoethyl)-N-(2-ammonioethyl) amino] diazen-1-ium-1, 2-diolate (DETA-NONOate) and bone marrow stromal cells promotes functional recovery. However,...
The aim of this study was to investigate the antioxidant and anti-inflammatory activities of aminoethyl-chitooligosaccharides (AE-COS) in murine microglial cells (BV-2). At the high concentration of 100 μg/ml, the inhibition of reactive oxygen species, DNA, protein and lipid oxidation were dete...
Poly(2-aminoethyl methacrylate) (PAMA) has a pKa of approximately 7.6 and is chemically stable in acidic or neutral aqueous solution in its protonated form. However, chemical degradation of PAMA is known to occur in alkaline media as its primary amine groups become deprotonated (He L et al. Macr...
In order to obtain compounds with modified 2-APB activities, we synthesized number of 2-APB analogues and analyzed their inhibitory activities for SOCE. The IC50 of 2-APB for SOCE inhibition is 3 μM while IC50 of some of our 2-APB analogues range 0.1–10 μM. The adducts of amino acids with dip...
Highly functionalized β-aminocyclohexanecarboxylate regio- and stereoisomers were synthetized from racemic unsaturated bicyclic β-lactams via enzymatic resolution, selective transformation of the C–C double bond by stereoselective epoxidation, and regioselective oxirane ring opening with azid...
A simple and novel method for the introduction of an extra hydroxy group into an aminocyclohexanecarboxylic acid via stereoselective epoxidation and regioselective opening of the oxirane ring is presented. This method permits the preparation of the enantiomerically pure hydroxylated amino acid.
A simple synthetic approach has been developed for the regio- and diastereoselective synthesis of hydroxylated 2-aminocyclohexanecarboxylic acid stereoisomers from 1,4-cyclohexadiene by the reductive opening of appropriate epoxide intermediates derived from the corresponding bicyclic β-lactams....
An overview of the methodologies that have been reported for the synthesis of furanoid and pyranoid sugar α- and β-amino acids and for the synthesis of related polyhydroxylated 1-amino and 2-aminocycloalkanecarboxylic acids from carbohydrates is presented herein.
Tranexamic acid (TXA) is a synthetic derivative of the amino acid lysine with antifibrinolytic properties. There is still a lack of pharmacokinetic and pharmacodynamic data concerning variable age groups undergoing surgeries with high blood loss. The optimum dose and administration schedules of ...
Stereoselective syntheses of racemic (1S,2R,3R,4R,5S,6R)- and (1S,2R,3R,4S,5S,6R)-3,4,5,6-tetrahydroxy derivatives of 2-aminocyclohexanecarboxylic acid have been achieved by a stereospecific Diels–Alder reaction between furan and maleic anhydride, a Curtius rearrangement and hydroxylation react...
A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs caused dose-dependent decreases in food intake and body weight in obese mice. Acute treatment with these compounds also led to a drop in ...
Fourier transform infrared spectra and Raman spectra of malonyl chloride methyl and ethyl esters, ClC(O)CH2C(O)OCH3 and ClC(O)CH2C(O)OC2H5, in the liquid phase were analysed. These spectra reveal the existence of diketo conformers. The theoretical calculations for ClC(O)CH2C(O)OCH3 at the HF3–2...
We have previously reported the discovery of small molecule inhibitors of malonyl-CoA decarboxylase (MCD) as novel metabolic modulators, which inhibited fatty acid oxidation and consequently increased the glucose oxidation rates in the isolated working rat hearts. MCD inhibitors were also shown ...
A series of heteroaryl-substituted bis-trifluoromethyl carbinols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Some thiazole-based derivatives showed potent in vitro MCD inhibitory activities and significantly increased glucose oxidation rates in isolated working rat...
A series of trifluoroacetophenone derivatives were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Some of the ‘reverse amide’ analogs were found to be potent inhibitors of MCD enzyme activity. The trifluoroacetyl group may interact with the MCD active site as the hydrate...
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