Search results for "DISCOVERY"
showing 10 items of 4119 documents
Racemische Histamin-H1-Agonisten
1984
Es wurden racemische α- und β-methylverzweigte 2-(2-Aminoethyl)-thiazole und 2-(2-Aminoethyl)-imidazole (Isohistamine) dargestellt und auf Histamin-H1- und -H2-agonistische Aktivitat gepruft. Histamine Analogues, XXVI: Racemic Histamine H1-Agonists Racemic α or β-methylated 2-(2-aminoethyl)thiazoles and 2-(2-aminoethyl)imidazoles (isohistamines) were prepared and tested for histamine H1- and H2-agonistic activity.
Histaminanaloge, 27. Mitt. Bis (2,2′-histamine)
1985
Es wurden p-Phenylen-bis(2,2′-histamin) (6a), Ethylen-bis(2,2′-histamin) (6b), Tetramethylen-bis(2,2′-histamin) (6c) und Hexamethylen-bis(2,2′-histamin) (6d) dargestellt und auf Histamin-H1-und H2-agonistische Aktivitat untersucht. Histamine Analogues, XXVII: Bis(2,2′-histamines) p-Phenylenebis(2,2′-histamine) (6a), ethylenebis(2,2′-histamine) (6b), tetramethylenebis(2,2′-histamine) (6c), and hexamethylenebis(2,2′-histamine) (6d) were prepared and tested for histamine H1,-and H2-agonistic activity.
Factors Affecting Hesitancy to mRNA and Viral Vector COVID-19 Vaccines among College Students in Italy
2021
Vaccine hesitancy (VH) may be significant in jeopardizing efforts to mass containment of COVID-19. A cross-sectional survey was carried out on a sample of 2667 Italian college students, before the COVID-19 vaccines became available for this age group (from 7 May to 31 May 2021). An online survey was created to obtain information about socio-demographic, health-related, and psychological factors linked to mRNA and viral vector COVID-19 vaccines. Statistically significant higher VH (30.4%) and vaccine resistance (12.2%) rates were found for viral vector than mRNA COVID-19 vaccines (7.2% and 1.0%, respectively; p < 0.001). Factors related to viral vector VH were partially different from tho…
The first sorbicillinoid alkaloids, the antileukemic sorbicillactones A and B, from a sponge-derived Penicillium chrysogenum strain
2005
The saltwater culture of a Penicillium chrysogenum strain isolated from the Mediterranean sponge Ircinia fasciculata yielded three new sorbicillin-derived compounds (1-3), whose structures were elucidated mainly by 2D NMR and mass spectrometry. Among them, sorbicillactones A (1) and B (2) are the first sorbicillinoid natural products that contain nitrogen. Compound 1 is anti-HIV active and it exhibits a strong cytotoxic activity against L5178y leukemic cells, combined with a relatively low toxicity to cervical carcinoma HeLa S3 cells and pheochromocytoma PC 12 cells. The absolute configurations of I and 2 were elucidated by quantum chemical calculation of circular dichroism (CD) spectra. An…
Stereocontrolled synthesis of D-α-hydroxy carboxylic acid from L-amino acids
1987
Abstract Optically active D-α-hydroxy carboxylic acids are obtained from L-amino acids via L-α-halocarboxylic acids and their stereoselective reaction with cesium p-nitrobenzoate.
Synthesis of tritium labeled 7α-methoxycarbonyl-15β,16β-methylene-3-oxo-17α-pregn-4-ene-21, 17-carbolactone, [3H]SH-D515, a highly selective tracer f…
1988
The synthesis of 7α-methoxycarbonyl-15β,16β-methylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone (5, SH-D515, ZK 91587), a potent aldosterone antagonist exhibiting a strong and very selective binding to the mineralocorticoid receptor and the tritiated analog 6 is reported.
Cytotoxic Activity and Composition of Petroleum Ether Extract from Magydaris tomentosa (Desf.) W. D. J. Koch (Apiaceae)
2015
The petroleum ether extract of Magydaris tomentosa flowers (Desf.) W. D. J. Koch has been analyzed by GC-MS. It is mainly constituted by furanocoumarins such as xanthotoxin, xanthotoxol, isopimpinellin, and bergaptene. Other coumarins such as 7-methoxy-8-(2-formyl-2-methylpropyl) coumarin and osthole also occurred. The antiproliferative activity of Magydaris tomentosa flower extract has been evaluated in vitro on murine monocye/macrophages (J774A.1), human melanoma (A375) and human breast cancer (MCF-7) tumor cell lines, showing a major activity against the latter.
H2-Antihistaminika, 15. Mitt.1) 1,n-Bis(2-imidazolyl)alkane
1983
Es wurden 1,n-Bis(2-imidazolyl)alkane mit Histamin-H2 funktionellen Seitenketten an C-4 der Imidazolringe dargestellt und auf H2-antihistaminische Aktivitat untersucht. H2-Antihistaminics, XV: 1,n-Bis(2-imidazolyl)alkanes 1,n-Bis(2-imidazolyl)alkanes with histamine H2-functional side-chains at C-4 of the imidazole rings were prepared and tested for H2-antihistaminic activity.
Nucleophilic benzoylation using a mandelic acid dioxolanone as a synthetic equivalent of the benzoyl carbanion. Oxidative decarboxylation of α-hydrox…
2004
The synthesis of alkyl aryl ketones using a mandelic acid dioxolanone as a synthetic equivalent (Umpolung) of the benzoyl carbanion is reported. The methodology involves alkylation of the mandelic acid dioxolanone, hydrolysis of the dioxolanone moiety in the alkylated products and oxidative decarboxylation of the resulting alpha-hydroxyacids. The last step is carried out in a catalytic aerobic way using a Co (III) complex in the presence of pivalaldehyde under very mild conditions.
Immunologische Grundlagen der allergischen Spätreaktion
1965
An transferaktiven Zellen von tb-sensibilisierten Tieren sind mindestens zwei distinkte zellstandige Antikorper nachweisbar. Eine Art dieser Antikorper ist gegen Tuberkulopolysaccharid und die andere gegen Tuberkuloprotein gerichtet. Sie haben beide nach Kontakt mit dem Antigen die Fahigkeit, Komplement zu binden. Eine Cytolyse kommt sowohl durch eine zellstandig ablaufende Immunreaktion zwischen Polysaccharid-Antikorper und Tuberkuloprotein-Antikorper mit dem Antigen zustande, jedoch ist dazu nur im letzteren Falle Komplement erforderlich. Nach Kontakt mit dem Antigen ist also beim Polysacharid-Antikorper eine Komplementbindung moglich, fur eine Cytolyse aber nicht notig. Die beiden zellst…