Search results for "Stereochemistry"
showing 10 items of 4831 documents
Struktur-Wirkungs-Beziehungen bei Histaminanaloga, 18. Mitt. Absolute Konfiguration und histaminartige Wirkung der Enantiomere von 5-Amino-4,5,6,7-te…
1979
Es werden die Racemattrennung von 5-Amino-4,5,6,7-tetrahydro-benzimidazol (3), die Bestimmung der absoluten Konfiguration sowie die histaminartige Wirksamkeit der Enantiomere am Ileum (H1) und Atrium (H2) des Meerschweinchens beschrieben. Structure-Activity Relationship of Histamine Analogues, XVIII: Absolute Configuration and Histamine-like Activity of the Enantiomers of 5-Amino-4,5,6,7-tetrahydrobenzimidazole The resolution of 5-amino-4,5,6,7-tetrahydrobenzimidazole (3), the determination of the absolute configuration and the histamine-like activity of the enantiomers on the guinea-pig ileum (H1) and atrium (H2) are reported.
Äther und Ester des 4-(2-Hydroxyaethyl)-imidazols und Ester der 4-Imidazolpropionsäure 4. Mitt. über Struktur-Wirkungs-Beziehungen bei Histaminanaloga
1974
Als potentiell histaminartig wirksame Substanzen wurden Ather und Ester des 4-(2-Hydroxyaethyl)-imidazols und Ester der 4-Imidazolpropionsaure dargestellt und am isolierten Ileum des Meerschweinchens und anderen Testobjekten untersucht. Ethers and Esters of 4-(2-Hydroxyethyl)-imidazole and Esters of 4-Imidazolepropionic Acid As substances with possible histamine-like activity, ethers and esters of 4-(hydroxyethyl)-imidazole and esters of 4-imidazolepropionic acid are prepared and tested on isolated guinea pig ileum and other objects.
Ester des 4-Hydroxymethyl-imidazols und der 4-Imidazolessigsäure 2. Mitt. über Struktur-Wirkungs-Beziehungen bei Histaminanaloga
1974
Als potentiell histaminartig wirksame Substanzen wurden Ester des 4-Hydroxymethyl-imidazols und der 4-Imidazolessigsaure dargestellt und am isolierten Ileum des Meerschweinchens und anderen Testobjekten untersucht. Esters of 4-Hydroxymethylimidazole and 4-Imidazoleacetic Acid As substances with possible histamine-like activity esters of 4-hydroxymethylimidazole and 4-imidazoleacetic acid were prepared and tested on isolated guinea-pig ileum and other objects.
ChemInform Abstract: Regioisomeric 5(3)-Aminomethyl-3(5)-phenylisoxazoles: Synthesis, Spectroscopic Discrimination, and Muscarinic Activity.
2010
The regioselective synthesis of isomeric 5(3)-aminomethyl-3(5)-phenyl isoxazoles using different methods is described. Spectroscopic data, especially mass spectrometric fragmentation, were used to identify and characterize the regioisomers. The muscarinic activity of these isoxazoles was assayed on isolated guinea-pig ileum and atria as well as on isolated rabbit vas deferens. Regioisomere 5(3)-Aminomethyl-3(5)-phenyl-isoxazole: Synthese, spektroskopische Unterscheidung und muskarinische Aktivitat Es werden verschiedene Verfahren zur regioselektiven Darstellung von 5(3)-Aminomethyl-3(5)-phenyl-isoxazolen beschrieben, die anhand ihrer spektroskopischen Daten, insbesondere der massenspektrosk…
Organochromium complexes - labelled aminoglycoside antibiotics derived from kanamycin A and tobramycin. Synthesis, structural characterization and us…
1993
Abstract The synthesis of metallocenic derivatives of aminoglycoside antibiotics, i. e. kanamycin A and tobramycin, is described. The organometallic-labelled compounds have been obtained from the reaction between the polyaminodrugs and organochromium esters of N-hydroxysuccinimide. The reaction proceeded selectively at the 6′-N position, as might be deduced both from the mass and the pH-dependent 13 C-NMR spectra. The procedure could be regarded as generally useful for the metallolabelling of aminoglycoside antibiotics. As an example of application a competitive immunoassay based on the use of these labels is proposed.
Tropane-derived11C-labelled and18F-labelled DAT ligands
2013
Radiolabelling of cocaine-derived 3-phenyltropanes for dopamine transporter positron emission tomography with 18F and 11C is reviewed. Copyright © 2013 John Wiley & Sons, Ltd.
Design, synthesis, DNA-binding and cytotoxicity evaluation of new potential combilexines
2002
Combilexines, compounds in which a DNA intercalator is linked to a minor groove binding component, interact with the DNA in a sequence specific manner to yield in most cases compounds with anticancer activity. A series of new compounds closely related to netropsin in which the two components were linked by an amide group was synthesised as potential combilexines. As some of these compounds showed cytotoxic activity in vitro, an attempt was made to rationalise their mechanism of action. The DNA binding characteristics of the carboxamides were evaluated by thermal denaturation experiments and by ethidium bromide displacement assay. Their ability to inhibit the topoisomerase I was also determi…
Stereoselective Synthesis of the Antiprotozoal Lactone Passifloricin A and Seven Isomers Thereof
2004
The conjugated delta-lactone passifloricin A, a natural product with antiprotozoal activity, and seven isomers thereof have been synthesized in enantiopure form. It has been shown in this way that the proposed structure for the natural compound was erroneous. The correct structure is now evidenced. Key steps of the syntheses were asymmetric Brown-type aldehyde allylations and ring-closing metatheses.
Correction: Total synthesis of two potent anti-inflammatory macrolactones of the oxacyclododecindione type
2015
Correction for ‘Total synthesis of two potent anti-inflammatory macrolactones of the oxacyclododecindione type’ by Johannes Tauber et al., Org. Biomol. Chem., 2015, 13, 7813–7821.
Synthesis, biological evaluation, and structure-activity relationship study of novel cytotoxic aza-caffeic acid derivatives.
2010
Abstract Three series of aza-caffeic acid derivatives with different linkers were designed and synthesized. Each of the synthesized derivatives was then used in cytotoxicity screening on either 8 or 12 human cancer cell lines. The structure–activity relationships on three structural regions A, B, and C are analyzed in detail, indicating that a nine bond linker B, containing a piperazine unit, is the most favorable linker leading to the generation of molecules with potent cytotoxicities. Compound ( E )-1-(4-(3,4-dichlorobenzyl)piperazin-1-yl)-3-(4-(4-ethoxybenzyloxy)-3,5-dimethoxyphenyl)prop-2-en-1-one ( 80 ) exhibited the most significant and selective cytotoxicity to KB, BEL7404, K562, and…