Search results for "medicinal"
showing 10 items of 2966 documents
Spectral characteristics of 5-hydroxymethylfurfural as a related substance in medicinal products containing glucose
2019
Objectives: To study 5-hydroxymethylfurfural (5-HMF) spectral characteristics aiming at their future application in analytical procedures and their validation for the determination of 5-HMF in liquid products containing glucose after sterilization.Method: Direct spectrophotometric method for the determination of 5-HMF using the molar absorption coefficient at the absorption maximum (284 nm).Results and discussion: aqueous 5-HMF solutions have strong absorption in the ultraviolet range below 310 nm and give two absorption maxima at wavelengths of 229–230 nm and 284 nm. An excellent linear relationship between absorbance and 5-HMF concentration was observed in the concentration range of 2.0–1…
Triazolopyridines 23. Synthesis of 5,5'-bi[1,2,3]triazolo[5,1-a]isoquinoline
2003
5,5'-Bi[1,2,3]triazolo[5,1-a]isoquinoline 6 has been synthesised from [1,2,3]triazolo[5,1-a] isoquinoline 5 by four procedures, dimerisation by LDA, Stille and Suzuki self-coupling reactions, and Suzuki cross-coupling reaction. The last is the best. Compound 6 gives 1,1'bi(acetoxymethyl)-3,3'-biisoquinoline 10 by triazolo ring opening by acetic acid.
Synthesis of substituted isoindolo[2,1-a]quinoxalin-6-yl–amino and 6-imino-5-yl thiourea derivatives
2014
A series of substituted 1-(5-bromopyridin-2-yl)-3-[2-(isoindolo[2,1-a]quinoxalin-6- ylamino)ethyl]thiourea and 1-(5-bromopyridin-2-yl)-3-[2-(6-iminoisoindolo[2,1-a]quinoxalin- 5(6H)-yl)ethyl]thiourea derivatives were prepared in good yields (63-85%) by reaction between the corresponding amino compounds with 5-bromo-2-isothiocyanatopyridine. All thiourea derivatives, tested for inhibition of HIV-1 RT, showed no significant antiviral activity.
Synthesis of pyrazole-4-carbohydrazide derivatives of pharmaceutical interest
2003
New 1-phenylor 1-methyl-5-benzamidopyrazole-4-carbohydrazide derivatives were prepared in 70–90% yields from 1-methylor 1-phenyl-6-phenylpyrazolo[3,4-d]1,3-oxazin-4(1H)-one derivatives and hydrazine hydrate. Small quantities of the isomeric 5-aminopyrazole-4-(Nbenzoyl)hydrazides were detected in some reaction mixtures, proving that intramolecular benzoyl migration can take place in the 5-benzamidopyrazole-4-carbohydrazide molecule. The direct formation of pyrazole-4-carbohydrazides from 5-benzamidopyrazole-4-carboxylic acid ethyl esters and hydrazine hydrate was unsuccessful.
Ruta chalepensis L. (Rutaceae) leaf extract: chemical composition, antioxidant and hypoglicaemic activities.
2017
Ruta chalepensis L. (Rutaceae) leaf extract was investigated for its chemical profile and antioxidant and hypoglycaemic properties. The antioxidant effects were investigated by 2,2-diphenyl-1-picrylhydrazyl (DPPH), Chi-carotene bleaching, and metal chelating activity assays. The carbohydrate-hydrolysing enzymes inhibition assay was used to test the hypoglycaemic potential. R. chalepensis showed a high content of hesperidin and rutin with values of 591.9 and 266.7 mg/g dry extract, respectively. The extract exhibited a promising protection of lipid peroxidation (IC50 value of 16.9 mu g/mL) and inhibited both alpha-amylase and alpha-glucosidase enzymes in a concentration-dependent manner. The…
Comparative chemical composition and bioactivity of leaves essential oils from nine Sicilian accessions of Myrtus communis L.
2019
In this study, the essential oils obtained from the leaves of Myrtus communis L. stored in a collection orchard located at the experimental station ‘Orleans’ of the Department of Agricultural and Forest Sciences of the University of Palermo (Italy) were investigated. The essential oils, analysed by gas chromatography–mass spectrometry, revealed the presence of α-pinene, 1,8-cineole, linalool, limonene and myrtenyl acetate as dominant constituents. The neuroprotective effects of M. communis essential oils were investigated by analysing the antioxidant properties and cholinesterases (acetylcholinesterase, AChE, and butyrylcholinesterase, BChE) inhibitory activity. Essential oils from Scopello…
Palladium-Catalyzed Direct Arylation of Heteroaromatics with Activated Aryl Chlorides Using a Sterically Relieved Ferrocenyl-Diphosphane
2012
International audience; The palladium-catalyzed direct arylations at C3 or C4 positions of heteroaromatics are known to be more challenging than at C2 or C5 positions. Aryl chlorides are also challenging substrates for direct arylation of heteroaromatics. We observed that in the presence of a palladium-catalyst combining only 0.5 mol % of Pd(OAc)2 with the sterically relieved new ferrocenyl diphosphane Sylphos, the direct arylation at C3 or C4 of oxazoles, a benzofuran, an indole, and a pyrazole was found to proceed in moderate to high yields using a variety of electron deficient aryl chlorides. Turnover numbers up to 176 have been obtained with this catalyst. Assessment of the electron-don…
Discovery of Retinoic Acid-Related Orphan Receptor γt Inverse Agonists via Docking and Negative Image-Based Screening
2018
Retinoic acid-related orphan receptor γt (RORγt) has a vital role in the differentiation of T-helper 17 (TH17) cells. Potent and specific RORγt inverse agonists are sought for treating TH17-related diseases such as psoriasis, rheumatoid arthritis, and type 1 diabetes. Here, the aim was to discover novel RORγt ligands using both standard molecular docking and negative image-based screening. Interestingly, both of these in silico techniques put forward mostly the same compounds for experimental testing. In total, 11 of the 34 molecules purchased for testing were verified as RORγt inverse agonists, thus making the effective hit rate 32%. The pIC50 values for the compounds varied from 4.9 (11 μ…
New cropping systems in semi-arid Mediterranean environments: potential role of medicinal and aromatic plants
2005
The semi-arid Mediterranean environments represent somehow “fragile” ecosystems, whose correct management needs some special attention. It is crucial therefore to study and point out some innovative farming systems able to deal with an income for workers, but in the meantime environmentally friendly and requiring the minimum energetic and technical inputs. In such sense, the cultivation of some selected medicinal and aromatic plants (MAPs) could be an important strategy. In our work we made an attempt to to sketch a comprehensive evaluation of the input levels required by 23 selected herbaceous MAPs, taking into consideration the indicative average levels of the energetic (including manpowe…
In vitro antitumor effects of the cold-water extracts of Mediterranean species of genus Pleurotus (higher Basidiomycetes) on human colon cancer cells
2014
The aim of this study was to evaluate whether the cold-water extracts of Pleurotus eryngii var. ferulae (CWE-Pef) and Pleurotus nebrodensis (CWE-Pn), 2 of the most prized wild and cultivated edible mushrooms, can affect the tumor phenotype of human colon cancer HCT116 cells. Our results showed that treatment with CWE- Pef and CWE-Pn resulted in a significant inhibition of the viability of HCT116 cells and promoted apoptosis, as also demonstrated by the increase of Bax-to-Bcl-2 messenger RNA ratio. Moreover, we observed that both extracts were able to inhibit cell migration and to affect homotypic and heterotypic cell-cell adhesion. It also was found that treatment with CWE-Pef and CWE-Pn ne…