N,N-Dimethylcarbamoylation of the anilinic nitrogen atom N(1) on the spiro 7-azaindoline consists of two steps. The first step is N,N-dimethylcarbamoylation of the pyridyl nitrogen atom N(7), leading to the formation of an isolable intermediate. The second step is intermolecular migration of the...

A range of β-aminonitriles (3-amino-3-phenylpropanenitrile and derivatives) were synthesised by reaction of various benzonitriles with acetonitrile and subsequent reduction of the resulting acrylonitrile products. These compounds were hydrolysed to the corresponding amides using the nitrile bio...

The radiotracer 3-[18F]fluoro-5-(2-pyridinylethynyl)benzonitrile, or [18F]FPEB, is a promising PET imaging agent for the metabotropic glutamate subtype 5 receptor (mGluR5). In an effort to develop a routine production method of this radiotracer for use in clinical research we adapted its radiosy...

Wine quality greatly depends on its chemical composition. Among the most important wine chemical compounds, flavonoids are the major contributors to wine organoleptic properties while amino acids have a huge impact on fermentation development and wine volatile profile. Likewise, nitrogen applica...

Chronic kidney disease (CKD) is a worldwide public health problem. Uremic retention solutes such as indoxyl sulfate (IS) and p-cresyl sulfate (PCS) are accumulated in CKD patients and are associated with the incidence of CKD progression. Amino acids are the major precursors of uremic retention s...

Mulberry (Morus alba L.) leaves are widely used as herbal tea to prevent heat stroke. Potential chemical markers of the antioxidant properties and its correlation with harvesting times and leaf location were explored in this study. A 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assay ...

AimsAntioxidant compounds have been extensively investigated as a pharmacological alternatives to prevent epileptogenesis. Rosmarinic acid (RA) and caffeic acid (CA) are compounds with antioxidant properties, and RA has been shown to inhibit GABA transaminase activity (in vitro). Our aim was to ...

Salvia miltiorrhiza Bunge is a traditional Chinese medicine, and its water-soluble phenolic acid active compounds have very important medicinal value; however, the synthesis pathways of the main active ingredients remain unknown. Here, we employed nuclear magnetic resonance (NMR)-based metabolom...

The effect of (D-Ala, D-Leu) enkephalin (DADLE) on the binding of GTP in hippocampal preparations was studied. It was observed that treatment of hippocampal slices with 10−5 −5×10−5 M DADLE followed by the preparation of membrane fractions reduced the binding of 35S-GTP-γ-S. There was no chang...

The research in the field of design and synthesis of unnatural amino acids is growing at a fast space for the increasing demand of proteins of potential therapeutics and many other diversified novel functional applications. Thus, we report herein the design and synthesis of microenvironment sens...

Solution syntheses of azapeptide pentamers 2, 3, and 4 were accomplished. The binding affinity of these azapeptides and azatide 1 were examined in the context of monoclonal antibody 3-E7 known to strongly bind the [Leu5]enkephalin sequence.

We studied antiarrhythmic action of d-Ala 2, Leu 5, Arg 6-enkephalin (dalargin) in experiments on male rats. Dalargin is reported to prevent heart rhythm disturbance and heart electrical stability decrease in experimental coronary occlusion, postinfarction, cardiosclerosis and emotional stress. ...

AimsFirst proof to show that (−)-deprenyl/selegiline (DEP), the first selective inhibitor of MAO-B, later identified as the first β-phenylethylamine (PEA)-derived synthetic catecholaminergic activity enhancer (CAE) substance and (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP), the try...

Antiserum to dynorphin B and antiserum to alpha-neoendorphin were used in an immunocytochemical examination of the guinea pig organ of Corti. Immunoreactive staining for these two proenkephalin B (prodynorphin)-derived peptides was seen in the lateral system of olivocochlear efferents in the org...

The synthesis of a new analog of adenosylhomocysteine (AdoHcy), 5′-deoxy-5′-(isobutylthio)-3-deazaadenosine, is described. The compound is a non-competitive inhibitor of AdoHcy hydrolase, with a Ki of 0.4 mM, as compared to a Ki of 3 μM for 3-deazaadenosine, a competitive inhibitor of the enz...

Phospholipid methylation in isolated hepatocytes was inhibited in the presence of 3-deazaadenosine (ID50 = 1.7 μM) 9-β-d-arabinofuranosyladenine (ID50 = 6.0 μM), S-tubercidinylhomocysteine (ID50 = 30 μM), and 5′-deoxy-5′-isobutylthioadenosine (ID50 = 177 μM). A transient inhibitory effect...

The spectroscopic properties of 3,5-difluorophenylboronic acid (3,5-DFPBA, C6H3F2B(OH)2) were investigated by FT-IR, FT-Raman UV–Vis, 1H and 13C NMR spectroscopic techniques. FT-IR (4000–400 cm–1) and FT-Raman spectra (3500–10 cm–1) in the solid phase and 1H and 13C NMR spectra in DMSO solu...

Possible stable conformers, geometrical molecular structures, vibrational properties as well as band assignments, nuclear magnetic shielding tensors of 2-Fluoro-3-Methylpyridine-5-Boronic Acid (2F3MP5BA) were studied experimentally and theoretically using FT-IR, Raman, (CP/MAS) NMR and XRD spect...

In this study, the experimental and theoretical vibrational frequencies of a newly synthesized 2,3,4,5,6-Pentafluoro-trans-cinnamic acid have been investigated. The experimental FT-IR (4000–400 cm−1) and Laser-Raman spectra (4000–100 cm−1) of the molecule in solid phase have been recorded. The...

The combination of palladium chloride with BINAP shows high efficiency in the decarboxylative cross-coupling reactions of arenecarboxylic acids with aryl iodides. The reactions proceed smoothly to generate the corresponding biaryl compounds in good to excellent yields.