In an effort to improve the oral bioavailability of naltrexone [17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6-one;1], a number of prodrug esters on the 3-hydroxyl group were prepared: the anthranilate (2), acetylsalicylate (3), benzoate (4), and pivalate (5). The oral bioavailabil...
The ground and excited states of naamine A, naamidine A and naamidine G have been investigated using the density functional theory and the time-dependent density functional theory methods. The geometric structures of naamine A, naamidine A and naamidine G in their ground and excited states are c...
Novak M. and Blackburn B. J. 1988. A nuclear magnetic resonance study of the d-[13C6]glucose metabolism of Mesocestoides corti tetrathyridia in the absence and presence of monensin. International Journal for Parasitology18: 1029–1033. The effect of monensin on the glucose metabolism of Mesocest...
Double Quantum (DQ) NMR, which utilizes the magnetic dipole interaction between the 13C atoms, was used for the complete assignment of the 13C NMR resonances to the corresponding carbon ring positions for the monoclinic and triclinic allomorphs of methyl 4′-O-methyl-β-d-cellobioside-13C12(1-13...
A systematic approach, which combines previously reported reactions with appropriate modifications, was established for preparing a variety of selectively deuterated nucleosides from glucose. We have developed a systematic method of synthesizing specifically deuterated nucleosides from glucose. ...
The preparation of 13C-labeled ribonucleosides starting from d-[13C6]glucose in 45% overall yield is described. The key of this short synthetic way is the dehomologation of di-O-isopropylidene hexofuranose 2 with periodic acid and NaBH4 that afforded stereoselectively the labeled ribofuranose de...
An isotopically labelled building block, 2,3,4,6-tetra-O-acetyl-1-thio-β-d-[13C6]glucopyranose (4), is obtained from the commercially available [13C6]-d-glucose. This hexa-13C-labelled thioglucose can be employed to make any glucosinolate (8) for use as an internal standard for isotopic dilutio...
Thirty extracts of plants traditionally used by the Chacobos, a native community living in the Amazonian part of Bolivia, were screened in vitro and/or in vivo for antimalarial activity. Two of the four species designated as antimalarial, Geissospermum laeve and Maquira coriacea, displayed rathe...
The present study was designed to isolate and characterize novel chemical constituents of the stem bark of Juglans mandshurica Maxim. (Juglandaceae). The chemical constituents were isolated and purified by various chromatographic techniques. The structures of the compounds were elucidated on the...
A new and stereoselective synthesis is described as an easy route to ostopanic acid using a versatile reagent : (2E,4E)-5-bromopentadienal.
Single crystal X-ray structure analysis of 5-(2-benzoimidazole-1-yl-ethoxy)-3-methyl-1-phenyl-1H-pyrazole-4-carboxylic acid methyl ester (2).0.5H2O provided experimental proof for H⋯OC, CH⋯OH and HO⋯N interactions. The embedded water molecule bridges between molecules 2 via non-covalent interact...
The series of 6-benzhydryl-4-methyl-2-(1H-benzoimidazol-2-yl)phenol derivatives (HL) and their zinc complexes (ZnL2) were synthesized and fully characterized. Single-crystal X-ray diffraction studies were conducted on representative complexes (C1 and C4), which revealed a distorted tetrahedral g...
Fibroblast growth factor receptor 1 (FGFR1) plays an important role in tumorigenesis and is therefore an attractive target for anticancer therapy. Using molecular docking approach we have identified inhibitor of FGFR1 belonging to 5-amino-4-(1H-benzoimidazol-2-yl)-phenyl-1,2-dihydro-pyrrol-3-one...
A practical direct preparation of tert-butyl esters from 2-tert-butoxypyridine has been developed. This system features the use of boron trifluoride·diethyl etherate in toluene solvent to rapidly achieve the reaction at room temperature. Using this reaction protocol, a variety of tert-butyl est...
Di- and tri-tert-butyl glycerol ethers (DTBGE and TTBGE) can be produced at high yields via etherification of glycerol with isobutene over cost effective and commercially available solid acid catalysts. These ethers have a potential to replace methyl-tert-butyl ether, an environmentally unfriend...
Diverse edible berries are native to the Patagonian region of Southern Chile. These berries are underused because their nutritional properties are relatively unknown. In this work, the profiles and concentrations of hydroxycinnamic acid derivatives and flavonols, and the antioxidant capacity of ...
A chemical investigation of the bark of Quercus stenophylla has led to the isolation and characterization of all of the possible structural isomers of quinic acid gallates; 3-O-, 4-O-, 5-O-, 3,4-di-O-, 3,5-di-O-, 4,5-di-O- and 3,4,5-tri-O-galloylquinic acids. Evidence for the structures of these...
In this work, quinoa and buckwheat cooked seeds were fermented by two autochthonous strains of lactic acid bacteria isolated from the corresponding seeds, namely Lactobacillus paracasei A1 2.6 and Pediococcus pentosaceus GS·B, with lactic acid chemically acidified seeds as control. The impact o...
Guiera senegalensis J.F. Gmel is a broad-spectrum African folk- medicinal plant, having activities against fowlpox and herpes viruses. Very recently, we have shown the anti-hepatitis B vius (HBV) potential of G. senegalensis leaves extract (GSLE). Here, we report the antioxidative and hepatoprot...
Six new gallotannins: 1-O- and 1,4-di-O-galloyl proto-quercitols, 1,4-di-O- and 1,3,4-tri-O-galloylquinic acids and 4-O- and 5-O-galloyl(−)-shikimic acids have been isolated from Quercus mongolica and Q. myrsinaefolia and their structures elucidated on the basis of chemical and spectroscopic evi...
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