Search results for "DISCOVERY"
showing 10 items of 4119 documents
Inhibitory effects on mitochondrial complex I of semisynthetic mono-Tetrahydrofuran acetogenin derivatives
2003
Modifications in the terminal alpha,beta-unsaturated gamma-methyl-gamma-lactone moiety or in the alkyl chain that links this terminal gamma-lactone with the alpha,alpha'-dihydroxylated THF system of the natural mono-tetrahydrofuranic acetogenins, annonacin and annonacinone, led to the preparation of eight semisynthetic derivatives. Their inhibitory effects on mitochondrial complex I is discussed and compared with that of the classical complex I inhibitor, rotenone.
Optimised procedures for the reversed-phase liquid chromatographic analysis of formulations containing tricyclic antidepressants.
2003
The chromatographic behaviour (retention, selectivity, peak shape and resolution) of seven tricyclic antidepressants (TCAs), amitryptiline, clomipramine, doxepin, imipramine, maprotiline, nortryptiline and trimipramine, was examined. Conventional unendcapped Cs and C18 columns and an endcapped XTerra MS C18 column recommended for the analysis of basic compounds were used together with acetonitrile-water and micellar sodium dodecylsulfate (SDS)-pentanol mobile phases. The two best combinations were XTerra C18/acetonitrile, which yielded the largest efficiencies and resolution, and C8/SDS-pentanol, which eliminated the peak tails that were still observed with the XTerra C18 column. Both the s…
Agrobacterium tumefaciens-mediated genetic transformation of the cardenolide-producing plant Digitalis minor L.
2003
A repeatable transformation system has been established for Digitalis minor using Agrobacterium tumefaciens. Leaf explants from 30-day-old seedlings were inoculated with either EHA105 (carrying the nptII and gusA genes) or AGL1 (with the bar and gusA genes) strains. Among the tested factors influencing T-DNA transfer to plants, the EHA105 strain and the addition of acetosyringone to the co-culture medium increased transformation. The highest transformation efficiency (8.4%) was obtained when freshly isolated explants, soaked in a bacterial suspension with an OD 550 of 0.9, were subcultured on selection medium after a 4-day co-culture with the bacteria. Evidence of stable transgene integrati…
Synthesis of 3-Oxa-guaianolides from Santonin
2000
Abstract This article reports on the transformation of santonin into two C10-epimeric 3-oxa-guaianolides which are 8-deoxyderivatives of several natural 3-oxaguaianolides isolated from Achillea species. The synthesis involved the photochemical rearrangement of the eudesmane skeleton into a guaiane skeleton and the transformation of the cyclopentane ring into a furan moiety with the concomitant loss of C3. Comparison of the NMR data of the synthetic products with those of the natural products confirms the β orientation of the hydroxyl group at C10 in the products isolated from Achillea.
Zur protonenkatalysierten Xanthenylierung von Tryptamin, Nω-Acetyltryptamin und Gramin: Ein Beitrag zur Konstitutionsaufklärung in der Indol-Analytik
1988
Zur protonenkatalysierten Aralkylierung von 1,2,3-Trimethylindol und 1,2,3,4-Tetrahydrocarbazol mit Arylaldehyden
1987
1,2,3-Trimethylindol (2) liefert mit Benzaldehyden die Kondensationsprodukte 5 und 6, wahrend aus den NH-Indolen 1 und 3 die Verbindungen 7 und 8 entstehen. Proton-catalyzed Aralkylation of 1,2,3-Trimethylindole and 1,2,3,4-Tetrahydrocarbazole with Arylaldehydes Reaction of 1,2,3-trimethylindole (2) with benzaldehydes leads to the condensation compounds 5 and 6, the NH-indoles 1 and 3, however, give 7 and 8.
Cladosins L-O, new hybrid polyketides from the endophytic fungus Cladosporium sphaerospermum WBS017
2019
Abstract The endophytic fungus Cladosporium sphaerospermum WBS017 was obtained from healthy bulbs of Fritillaria unibracteata var. wabuensis. Fermentation of C. sphaerospermum on solid rice medium yielded three new hybrid polyketides, cladosins L−N (1–3), and a known derivative cladodionen (4). Further cultivation of this fungus on white bean medium afforded an additional new hybrid polyketide, cladosin O (5) along with three known analogues (6–8). The structures of the new compounds were elucidated using a combination of NMR and HRESIMS data. The absolute configurations of compounds 2 and 3 were determined by Mosher’s method and TDDFT-ECD calculations. All isolated compounds were evaluated…
Short and Efficient Chemoenzymatic Synthesis of Goniothalamin.
2004
A high-yielding three-step synthesis of goniothalamin involving an enzymatic kinetic resolution in the presence of vinyl acrylate followed by ring-closing metathesis is discussed.
Application of LA-ICP-MS as a rapid tool for analysis of elemental impurities in active pharmaceutical ingredients.
2014
The control of inorganic contaminants in active pharmaceutical ingredients has a significant role in the quality control of drug products. The concentration limits for metal residues in drug products have been defined by various regulatory guidelines. Laser ablation inductively coupled plasma mass spectrometry (LA-ICP-MS) is a powerful and fast analytical technique for multi-elemental analysis. A disadvantage in using LA-ICP-MS method is the lack of matrix reference materials for validation and calibration purposes. This article focuses on the handling strategy of laboratory-made matrix calibration standards for the quantification of elemental impurities in an active pharmaceutical ingredie…