Novel diimidazo[1,2-a:5′,1′-c]quinoxaline derivatives were synthesized by a Pd-catalyzed intramolecular coupling reaction of 1,2-bis(2-iodo-1H-imidazol-1-yl)benzene. This method was applied to the selective introduction of an aryl substituent at the 10 position by the addition of a boronic est...

The active sites of feruloyl esterases from mesophilic and thermophilic sources were probed using methyl esters of phenylalkanoic acids. Only 13 out of 26 substrates tested were significant substrates for all the enzymes. Lengthening or shortening the aliphatic side chain while maintaining the s...

Protein tyrosine phosphatase 1B (PTP1B) has been considered as a promising therapeutic target for type 2 diabetes mellitus (T2DM) and obesity due to its key regulating effects in insulin signaling and leptin receptor pathways. In this work, a series of cis- and trans-pyrrolidine bisarylethenesul...

A novel route was created to facilitate the degradation of diethyl phthalate (DEP) upon micellar polyoxometalate (POM) catalysts and H2O2. The best catalytic activity was obtained using [C16H33N(CH3)3]H4PMo10V2O40 (N-hexadecyl-N,N,N-trimethylammonium tetrahydrogen decamolybdo-divanadophosphate, ...

New general and operationally simple method for preparation of racemic diethyl α-fluoro-β-ketophosphonates has been developed. Addition of LDA to solution of diethyl fluoromethylphosphonate and aromatic, heteroaromatic and aliphatic esters in THF at −78 °C afforded the corresponding diethyl α...

The effect on wash fastness of aftertreating the dyeings of six C.I. Solubilised Sulphur dyes on cotton with a proprietary, reactive, cationic fixing agent was examined. The fixing agent improved wash fastness when applied to the oxidised dyeings and also when applied to the leuco derivative of ...

A multi-cathode electrolyser was used for the direct cathodic reduction of oxidised, dispersed C.I. Sulphur Black 1. Crude C.I. Sulphur Black 1 at concentrations of 80 g L−1 and 131 g L−1 could be reduced using a cathodic current density of 5.3 mA cm−2. During reduction at pH 12.2–12.6 the redo...

We synthesized five iron chelator derived from 2,6-diacetylpyridine bis(acylhydrazones) and proved their iron complexes structure by X–ray single crystal diffraction. These ligands have a significant anticancer proliferative activity and low cytotoxicity against normal cells. The Fe(III) comple...

Several Mannich bases derived from conjugated styryl ketones were shown to have potent cytotoxicity toward murine leukemia L-1210 cells and Walker 256 carcinosarcoma cells in culture. The most cytotoxic derivative, (E)-1-(3,4-dichlorophenyl)-4-dimethylaminomethyl-1-nonen-3-one hydrochloride, pro...

(±)-1-Acyl-3-(3,4-dichlorophenyl)-3-[2-(spiro-substituted piperidin-1′-yl)ethyl]piperidines and their quaternary ammonium salts were prepared and evaluated for their NK1 receptor antagonistic activity. Some of these inhibited SP-induced contraction in guinea pig ileum with IC50 values at a lev...

The synthesis of impurities detected in clandestinely manufactured Amphetamine Type Stimulants (ATS) has emerged as more desirable than simple “fingerprint” profiling. We have been investigating the impurities formed when phenyl-2-propanone (P2P) 5, a key ATS precursor, is synthesised in three...

Electronic absorption spectra of 2-methylamino-, 2-ethylamino-3-methyl-4-nitropyridine and 2-ethylamino-, 2-methylamino-5-methyl-4-nitropyridine in the solid state and ethyl alcohol solution have been measured at room temperature. Their luminescence spectra and life times have been recorded at r...

Targeting CDK4/6 has been identified as an effective therapeutics for treatment of cancer. We herein reported the discovery of a series of 6-(2-(methylamino)ethyl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine derivatives as CDK4/6 inhibitors against cancer. Compound 3c, which displayed high poten...

The Schiff base compound (Z)-4-methyl-N-[2-((2-oxonaphthalen-1(2H)-ylidene)methylamino)ethyl]-benzenesulfonamide has been synthesized and characterized by IR, UV–Vis and single-crystal X-ray diffraction. Molecules of the title compound exist as NH tautomeric form in solid state. Molecular geome...

Tow new α-aminophosphonic acids, Ethyl hydrogen [(2-methoxyphenyl)(methylamino) methyl]phosphonate (2-EHMAP) and Ethyl hydrogen [(3-methoxyphenyl)(methylamino) methyl]phosphonate (3-EHMAP) were synthesized by the reaction between Methylamine, 2- or 3-Methoxybenzaldehyde and Diethylphosphite in ...

The development of a new fluorous-tagged ammonia-equivalent for the synthesis of N-alkylated amino acids is described. The required building blocks were readily accessed in high yield and purity using F-SPE purification technique. Coupling of the fluorous-tagged hydroxylamines with a selection o...

The preparatin of N,N,O-tris(trimethylsilyl)hydroxylamine by silylation of hydroxylammonium sulfate and its chemical and physical properties are described. The IR, Raman and 1H NMR Spectra of this compound and of tris(trimethylsilyl)hydrazine are reported and discussed.

Fluoro- und aminofluoro-silanes react with the lithium salt of N,O-bis(trimethylsilyl)hydroxylamine under LiF elimination and substitution. Alkyl- and amino-fluorosilanes give O-fluorosilyl-N,N-bis(trimethylsilyl)hydroxylamines, arylfluorosilanes give N-fluorosilyl-N,O-bis(trimethylsilyl)hydroxy...

The lithium derivative of N,O-bis(tert-butyldimethylsilyl)hydroxylamine, Me3CSiMe2NHOSiMe2CMe3 (1), is isolated as the first dimeric O-lithium-N,N-bis(silyl)hydroxylamide, [(THF)LiON(SiMe2CMe3)2]2 (2). The tendency of the hard Lewis-acid lithium to bind the hard Lewis-base oxygen explains ...

Vascular adhesion protein-1 (VAP-1) is a promising therapeutic target for the treatment of diabetic nephropathy. Here, we conducted structural optimization of the glycine amide derivative 1, which we previously reported as a novel VAP-1 inhibitor, to improve stability in dog and monkey plasma, a...