The excitatory amino acids (EAA) l-glutamate (l-Glu), l-aspartate (l-Asp) and d-aspartate (d-Asp) are thought to play a neurotransmitter/neuromodulator role in neuronal communications. Recently, a high level of EAA l-Glu, d- and l-Asp isomers has been found in the forebrain of Naples high-excita...

Series of N-substituted diethyl aspartates and N-substituted-3-oxo-1, 4-piperazine-2-acetic acid esters were synthesized as potential inhibitors of aspartate transcarbamoylase. The aspartates were obtained by addition of substituted alkyl amines to diethyl maleate, or conversion of the hydroxy e...

Dihydroxyacetone sulfate is a substrate for α-glycerolphosphate dehydrogenase (sn-glycerol-3-phosphate:NAD + 2-oxidoreductase, EC 1.1.1.8). The substitution of the sulfate for the phosphate does not affect the Km of the enzyme for NADH. It affects, on the contrary, the Km of the sugar ester, wh...

The biodiesel industry generates glycerol as a main by-product, and the conversion of glycerol to value-added products is an important issue. Glycerol dehydrogenase (GDH) can catalyze the conversion of glycerol to dihydroxyacetone (DHA), which is used as a tanning agent in cosmetics and is much ...

A simple and effective high-performance liquid chromatography with diode-array detection method coupled with a liquid-liquid extraction pretreatment has been developed for determining the pharmacokinetics and tissue distribution of a novel structurally modified derivative (8-acetamino-isocorydin...

The asymmetric total synthesis of (S)-isocorydine, a potential drug for the cure of hepatocellular carcinoma, is described. Asymmetric transfer hydrogenation of 3,4-dihydroisoquinoline using a chiral Ru(II) catalyst was applied to the synthesis of isocorydine as the key step, in which the ee val...

Racemization of R-2-amino-1-butanol proceeded effectively over a fixed-bed Raney cobalt catalyst in a continuous fixed-bed reactor under the hydrogen pressure in the range of 2.0–6.0 MPa. The performance of a fixed-bed Raney cobalt catalyst was compared with that of a pulverous Raney cobalt cat...

The synthesis of 47 structurally diverse compounds incorporating the (R)-2-amino-1-butanol motif has been realized. Ten of these compounds were found to exhibit in vitro specific activity against Mycobacterium tuberculosis H37Rv in a MIC range of 0.65 μM–14.03 μM. Five of the most active comp...

The synthesis of 22 structurally diverse urea, thiourea and acylthiourea derivatives containing the (R)-2-amino-1-butanol motif has been performed. The evaluation of their in vitro activity against Mycobacterium tuberculosis (H37Rv and strain 43) showed promising results in the case of the acylt...

The intercellular lipid matrix of the stratum corneum (SC), which consist mainly of ceramides (CERs), free fatty acids and cholesterol, is fundamental to the skin barrier function. These lipids assemble into two lamellar phases, known as the long and short periodicity phases (LPP and SPP respect...

A straightforward synthesis of l-lyxo- and l-xylo-phytosphingosine along with their isomeric analogues has been accomplished. The salient features of this approach are the utilization of [3,3]-sigmatropic rearrangements to install a C-N bond and application of a late stage Wittig or OCM reaction...

A simple and efficient protocol for the synthesis of a sphingosine starting from cost-effective phytosphingosine has been described. Two alternative synthetic pathway have been disclosed based on the use of two different kinds of protective groups for the protection of the amino group in the phy...

Two new series of imidazole derivatives (acetamides: 1–8 and sulfonamides: 9–15) were synthesized using a short synthetic route. Compound 1 as well as the intermediate 16g were characterized by X-ray crystallography. Imidazole derivatives 1–15 were tested in vitro against three unicellular pa...

IntroductionNitroimidazole (azomycin) derivatives labeled with radioisotopes have been developed as cancer imaging and radiotherapeutic agents based on the oncological hypoxic mechanism. By attaching nitroimidazole core with different functional groups, we synthesized new nitroimidazole derivati...

The design, synthesis, in vitro and in vivo evaluation of 5-nitro benzimidazole with 1,4-disubsituted or 1,5-disubsituted indole derivatives as novel angiotensin II receptor antagonist is outlined. Radioligand binding assays showed that 2-(4-((2-butyl-5-nitro-1H-benzo[d]imidazol-1-yl)methyl)-1H-...

Chemical studies have indicated that, following reduction of misonidazole to the hydroxylamine derivative, reaction with guanosine leads to the formation of a 2-carbon addition product of guanosine. In this study, the formation of the guanosine product is used to detect the presence of a reactiv...

IntroductionDevelopment of new 18F-labeled tracers for positron emission tomography (PET) imaging is increasingly important. Herein, we described the synthesis of silicon analogues of [18F]fluoromisonidazole in order to develop new radiolabelled compounds for the detection of tumour hypoxic doma...

β-Laminaribiose octaacetate (2b) was prepared in greater than 50% yield from the microbial polysaccharide curdlan by specific degradation with a yeast cell-wall lytic enzyme preparation, Kitalase, and subsequent acetylation. Acetolysis of curdlan also gave α-laminaribiose octaacetate (2a) in 2...

High-purity, erbium hydride thin films have been deposited onto α-Al2O3 and oxidized Si by reactive sputtering methods. Rutherford backscattering spectrometry and elastic recoil detection show that films deposited at temperatures of 35, 150 and 275 °C have a composition of 3H:1Er. Erbium trihy...

Erbium was used as a model hydride-forming metal to study the possibility of applying thermal desorption spectroscopy (TDS) to research into hydride decomposition. The possibility of varying heating rates and final temperatures makes TDS acceptable for providing experimental information about th...