A sensitive UPLC–MS/MS method was established for the simultaneous determination of seven fluorescent whitening agents in flour matrix. Samples were ultrasonically extracted by trichloromethane-acetone. Then analytes were separated on a C18 column and detected by MS/MS. The developed method was...

Nitroxyl (HNO), generated from nitric oxide (NO) in biological system, plays distinct biological roles in physiological process, but the role of endogenous HNO in biosystems still remains unclear, because of lacking of specific and sensitive detector to monitor HNO in real time. The conventional...

Edible mushrooms are valued because of their umami taste and good nutritional values. Free amino acids, 5′-nucleotides and nucleosides were analyzed from four Nordic forest mushroom species (Lactarius camphoratus, Boletus edulis, Cantharellus cibarius, Craterellus tubaeformis) using high precis...

Raman spectra have been obtained for 1-methyladenosine-5′-phosphate in H2O and D2O over a wide pH range, and its rearrangement in mild alkali to N6-methyladenosine-5′-phosphate has been followed. Similarly, the spectra of tubercidin (7-deazaadenosine) and 1-methyltubercidin were measured and t...

Alzheimer's disease pathomimetic toxicity could be induced in mice within one week after the intracerebroventricular (i.c.v.) injection of an aggregated preparation of the highly toxic and endogenous amyloid-β fragment Aβ25–35. It was recently reported that Aβ25–35 also provokes a modi...

A series of trans-N-alkyl-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and characterized for binding and function at the melanocortin-4 receptor (MC4R), and several potent benzylamine derivatives were identified. Compound 18v was found to bind...

The identification of a series of sulfonyl-amino-acetamides as BACE-1 (β-secretase) inhibitors for the treatment of Alzheimer’s disease is reported. The derivatives were designed based on the docking simulation study, synthesized and assessed for BACE-1 inhibition in vitro. The designed ligand...

2-Methylquinoline promoted room-temperature oxidative ring-opening of N-sulfonyl aziridines with DMSO has been developed, providing a mild and convenient method for the synthesis of a variety of different N-sulfonyl protected α-amino aryl ketones. The employment of 2-methylquinoline was crucial...

For the purpose of synthesizing drug candidates with desirable bioactivity, a class of benzoyl amide containing nitrogen heterocyclic ring derivatives targeting VEGFR-2 was designed and screened out using Discovery Studio. Eighteen target compounds were synthesized and then selected by some biol...

A series of novel α-sulfonyl γ-(glycinyl-amino)proline peptidomimetic derivatives were designed, synthesized and assayed for their activities against matrix metalloproteinase-2 (MMP-2), aminopeptidase N (APN)/CD13 and HDACs. The results indicated that all the compounds exhibited highly selecti...

The synthesis of derivatives of 2-(1-an-aminoalkyl)-4-carboxy-3,4,5,6-tetrahydropyrimidines, unusual amino acids isolated from bacterial siderophores, is described, from condensation of N-protected amino acids imidates or thiomidates with 2,4-diaminobutyrylglycine methyl ester.

Bis(1-methylimidazol-2-yl)methane and 1-(1-methylimidazol-2-yl)methyl-3,5-dimethylpyrazole [CH2(min)(pz)] could be deprotonated with n-BuLi at the bridging carbon atom. The corresponding anions were inactive in the reaction with Ph3SnCl but reacted with sulfur, followed by reaction with Ph2SnCl2...

A new series of aromatic ester and carbamate derivatives of 2-(1H-imidazol-1-yl)-1-phenylethanol were synthesized and evaluated for their antifungal activity towards Candida albicans and non-albicans Candida species strains. The aromatic biphenyl ester derivatives 6a–c were more active than the...

Pure-component vapor pressure of 3-methylpentane and vapor–liquid equilibrium (VLE) for the binary systems of 3-methylpentane with methyl 1,1-dimethylethyl ether (MTBE) and with methyl 1,1-dimethylpropyl ether (TAME) at 101.3 kPa have been measured. Both systems exhibit small positive deviation...

The excess molar enthalpies of (acetonitrile  +  1,1-dimethylethyl methyl ether) and (methanol, or ethanol  +  acetonitrile  +  1,1-dimethylethyl methyl ether) have been measured atT = 298.15 K and atmospheric pressure using a flow microcalorimeter. The experimental results are correlated with p...

Each stereoisomer of 3-[methyl(1,2,3,4-tetrahydro-2-naphthalenyl)amino]-1-indanone, 1a–d, was prepared and evaluated in vitro for its ability to prevent mediator release induced by different degranulating agents from rodent mast cells and also in vivo against passive cutaneous anaphylaxis. The ...

We have previously reported the discovery of a new class of potent inhibitors of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) derived from benzylidene oxazolidinedione and thiazolidinedione scaffolds. In this study, these analogs were designed, synthesized, and evaluated in a human cell-...

N-Phosphoryl amino acids were prepared rapidly and in high yield via phosphoramidite amine-exchange in the presence of 1H-tetrazole followed by oxidation with mCPBA. Formation of dibenzyl phosphoramidates incorporating the representative C-terminal protected amino acids leucine, phenylalanine, g...

In vitro anti-resorptive activity, mechanism of action, pharmacokinetic profile and in vivo anti-resorptive activity of N1,N1-diisopropyl-N2-(diphenylphosphoryl)-2-(4-nitrophenyl)acetamidine (1) were evaluated.

The structural characteristics of N-phosphoryl branched peptides 2–5 in solution were investigated by NMR spectroscopy. We observed diastereotopic phenomena, interactions between hydrogen bonds and lack of regular secondary structure in these peptides. We also conducted conformational analysis ...