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  • 1
    Electronic Resource
    Electronic Resource
    Effects of the class III antiarrhythmic drug ambasilide on outward currents in human atrial myocytes (1996)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 353 (1996), S. 226-232 
    Details
    ISSN: 1432-1912
    Keywords: Human atrial myocytes ; Transient outward current ; Sustained outward current ; Class III antiarrhythmic drug ; Ambasilide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We have studied the inhibitory influence of the class III antiarrhythmic drug ambasilide (LU 47110) on the transient outward current I to1 and the sustained current T so following inactivation of I to1 in human atrial myocytes. The two currents are separated by a mathematical procedure based on the amplitudes and time constants of the biexponential inactivation of the total outward current. The frequency dependence, the recovery from inactivation and the kinetics of activation and inactivation are described. Ambasilide reversibly and concentration dependently inhibited I to1, I so and the sodium current I Na. Concentration required for half maximal inhibition (IC50) for the effects on I to1 and I so were 23.3 μmol/l and 45.7 μmol/l respectively, concentrations shown by others to be effective in terminating and preventing fibrillation in a dog atrial arrhythmia model. Ambasilide not only reduced the amplitude of I to1 and I so but also accelerated the time course of inactivation from 14.22 to 6.69 ms and from 202.3 to 87.9 ms respectively. The amplitude of I to1 showed only a small dependence on stimulation frequency characteristic for human atrial myocytes, whereas I so was reduced significantly at higher stimulation frequencies. Ambasilide did not change these relationships (0.1–4 Hz) and therefore did not show the reverse use-dependence known from other class III antiarrhythmic agents and which is an important property for a prospective antiarrhythmic drug. The lack of an effect of ambasilide on both steady-state activation and inactivation of I to1, and the time constant of recovery from inactivation, suggests that ambasilide acts by changing conductance rather than by influencing the gating mechanism. The described characteristics make ambasilide an interesting substance in the group of class III antiarrhythmic drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00168761
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  • 2
    Electronic Resource
    Electronic Resource
    Effects of the class III antiarrhythmic drug ambasilide on outward currents in human atrial myocytes (1996)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 353 (1996), S. 226-232 
    Details
    ISSN: 1432-1912
    Keywords: Key words Human atrial myocytes ; Transient outward current ; Sustained outward current ; Class III antiarrhythmic drug ; Ambasilide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  We have studied the inhibitory influence of the class III antiarrhythmic drug ambasilide (LU 47110) on the transient outward current I to1 and the sustained current I so following inactivation of I to1, in human atrial myocytes. The two currents are separated by a mathematical procedure based on the amplitudes and time constants of the biexponential inactivation of the total outward current. The frequency dependence, the recovery from inactivation and the kinetics of activation and inactivation are described. Ambasilide reversibly and concentration dependently inhibited I to1, I so and the sodium current I Na. Concentration required for half maximal inhibition (IC50) for the effects on I to1 and I so were 23.3 μmol/l and 45.7 μmol/l respectively, concentrations shown by others to be effective in terminating and preventing fibrillation in a dog atrial arrhythmia model. Ambasilide not only reduced the amplitude of I to1 and I so but also accelerated the time course of inactivation from 14.22 to 6.69 ms and from 202.3 to 87.9 ms respectively. The amplitude of I to1 showed only a small dependence on stimulation frequency characteristic for human atrial myocytes, whereas I so was reduced significantly at higher stimulation frequencies. Ambasilide did not change these relationships (0.1–4 Hz) and therefore did not show the reverse use-dependence known from other class III antiarrhythmic agents and which is an important property for a prospective antiarrhythmic drug. The lack of an effect of ambasilide on both steady-state activation and inactivation of I to1, and the time constant of recovery from inactivation, suggests that ambasilide acts by changing conductance rather than by influencing the gating mechanism. The described characteristics make ambasilide an interesting substance in the group of class III antiarrhythmic drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00168761
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  • 3
    Electronic Resource
    Electronic Resource
    1-Aryl-1-heterosubstituierte λ5-Phosphorine durch Arylierung von λ3-Phosphorinen mit Aryldiazoniumsalzen in Gegenwart von Nucleophilen (1975)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 108 (1975), S. 3271-3280 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis of 1-Aryl-1-hetero-substituted λ5-Phosphorins by Arylation of λ3-phosphorins with Aryldiazonium Salts in the Presence of Nucleophiles2,4,6-Trisubstituted λ3-phosphorins react in acetonitrile or dimethoxyethane with aryldiazonium tetrafluoroborates to give 1-aryl-1-fluoro-λ5-phosphorins 4 (Nu = F). In the presence of alcohols or phenols 1-alkyloxy (or 1-aryloxy)-1-aryl-λ5-phosphorins 4 (Nu = OR) are produced; in the presence of water 1,1′-oxybis(1-aryl-λ5-phosphorins) 10 are formed. The latter can also be transformed into 1-alkoxy(or 1-aryloxy-)-1-aryl-λ5-phosphorins 4 (Nu = OR) by nucleophilic displacement with alcohols or phenols. With alkanthiols in the presence of Lewis acids 1-alkylthio-1-aryl-λ5-phosphorins 11 (Nu = SR) are produced, which are inaccessible by the former method. The mechanism is discussed especially in connection with some unexpected products which were observed.
    Notes: Bei der Umsetzung von 2,4,6-trisubstituierten λ3-Phosphorinen mit Aryldiazonium-tetrafluoroboraten in Acetonitril oder Dimethoxyäthan entstehen 1-Aryl-1-fluor-λ5-phosphorine 4 (Nu = F). In Gegenwart von Alkoholen und Phenolen bilden sich 1-Alkoxy(bzw. 1-Aryloxy)-1-aryl-λ5-phosphorine 4 (Nu = OR), in Gegenwart von Wasser 1,1′-Oxybis(1-aryl-λ5-phosphorine) 10. Letztere können durch nucleophile Verdrängung mit Alkoholen oder Phenolen ebenfalls in 1-Alkoxy-(bzw. 1-Aryloxy)-1-aryl-λ5-phosphorine 4 (Nu = OR) übergeführt werden; mit Alkanthiolen in Gegenwart von Lewis-Säuren entstehen nach dem ersten Verfahren nicht zugängliche 1-Alkylthio-1-aryl-λ5-phosphorine 11 (Nu = SR). Der Mechanismus wird insbesondere im Zusammenhang mit einigen beobachteten, unerwarteten Reaktionsprodukten diskutiert.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19751081017
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  • 4
    Electronic Resource
    Electronic Resource
    Arylierung von λ5-Phosphorinen mit Aryldiazoniumsalzen (1975)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 108 (1975), S. 3281-3285 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Arylation of λ5-Phosphorins with Aryldiazonium Saltsλ5-Phosphorin derivatives with a phenyl residue at C-4 are arylated by aryldiazonium salts in benzene/methanol in the 4-phenyl ring with elimination of nitrogen: even when the aryl-residue at C-4 is substituted by a phenolic hydroxyl group arylation with elimination of the hydroxyl group and not azo coupling occurs. 2,4,6-Tri-tert-butyl-1,1-diphenoxy-λ5-phosphorin, however, reacts with an aryldiazonium salt by electrophilic replacement of the tert-butyl group at C-4 to give the arylazo dye of the λ5-phosphorin (20).
    Notes: λ5-Phosphorin-Derivate, die einen Phenylrest an C-4 tragen, werden durch Aryldiazoniumsalze in Benzol/Methanol unter Abspaltung von Stickstoff im 4-Phenylring aryliert; selbst wenn dieser Phenylrest an C-4 durch eine phenolische Hydroxylgruppe substituiert ist, tritt Arylierung unter Verdrängung der Hydroxylgruppe und nicht Azokupplung ein. 2,4,6-Tri-tert-butyl-1,1-diphenoxy-λ5-phosphorin dagegen kuppelt mit einem Aryldiazoniumsalz im Sinne einer elektrophilen Substitution unter Verdrängen der tert-Butylgruppe an C-4 zu dem Arylazofarbstoff des λ5-Phosphorins (20).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19751081018
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  • 5
    Electronic Resource
    Electronic Resource
    Bimolecular Formation of Radicals by H-Transfer, 6. Uncatalyzed Transfer Hydrogenation of a Benzhydryl Fluoride by 9,10-Dihydroanthracene (1994)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 127 (1994), S. 557-563 
    Details
    ISSN: 0009-2940
    Keywords: Hydrogen transfer ; Molecule-induced radical formation ; Reduction of C—F bond ; 1-Adamantylfluorodiphenylmethane ; Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: 1-Adamantylfluorodiphenylmethane (2) was reduced to 1-adamantyldiphenylmethane (3) when heated with 9,10-dihydroanthracene to 330°C. From the second-order kinetics, the activation parameters (ΔH
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19941270316
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  • 6
    Electronic Resource
    Electronic Resource
    Thermische Umlagerungen von 1-Allyloxy- und 1-Propargyloxy λ5-phosphorin-Derivaten (1981)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 114 (1981), S. 1752-1766 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Thermal Rearrangements of 1-Allyloxy- and 1-Propargyloxy-λ5-phosphorin DerivativesThe thermal rearrangements of 1-allyloxy-λ5-phosphorin derivatives 1 affords - contrary to the formally similar Claisen rearrangement of allyl phenyl ethers - in the irreversible step an “anti-Woodward-Hoffmann” [3s5s] allyl shift to 4-allyl-1,4-dihydro-λ5-phosphorin derivatives 2. - The reaction is, as cross experiments prove, intramolecular and stereospecific according to 1st order law. It is accelerated by electron donating substituents in position 4 and by electron attracting substituent at the phosphorus, but is not much solvent-dependant. In a next step, again with allyl-inversion, a [3s3s] Cope rearrangement follows to give 2-allyl-1,2-dihydro-λ5-phosphorin derivatives 3. At somewhat higher temperature, by an intramolecular [4 + 2]-cycloaddition from 3j a tricyclus 4 is formed. Besides the experiments with deuterium marked compounds, the X-ray analysis of 4 proves the uniform stereochemic way of all these rearrangements. Steric and electronic influences on some analogous rearrangements are studied, the mechanism is discussed.
    Notes: Die thermische Umlagerung von 1-Allyloxy-λ5-phosphorin-Derivaten 1, führt im Gegensatz zu der formal ähnlichen Claisen-Umlagerung von Allylphenylethern im irreversiblen Primärschritt in einer“ anti-Woodward-Hoffmann”-[3s5s]-Allylwanderung zu 4-Allyl-1,4-dihydro-λ5-phosphorin-Derivaten 2. -Die Reaktion verläuft, wie Kreuzungsexperimente beweisen, intramolekular und stereospezifisch nach einer Reaktion 1. Ordnung. Sie wird durch elektronenabgebende Substituenten in R4 und elektronenanziehende substituenten am Phosphor gefördert, ist jedoch wenig löungsmittelabhängig. Ihr folgt in einem irreversiblen Schritt unter erneuter Allyl-Umkehr eine [3s3s]-Cope-Umlagerung zu 2-Allyl-1,2-dihydro-λ5-Phosphorin-Derivaten 3. Bei etwas höherer Temperatur gehen diese eine intramolekulare [4 + 2]-Cycloaddition zum Tricyclus 4 ein. Dessen Röntgenstrukturanalyse sowie die eindeutigen Deuterierungsergebnisse sprechen für einen stereochemisch einheitlichen verlauf der Umlagerungen. Sterische und elektronische Einflüsse auf einige analoge Umlagerungen werden untersucht, der Mechanismus wird diskutiert.
    Additional Material: 4 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19811140515
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  • 7
    Electronic Resource
    Electronic Resource
    Gleitringdichtungen für Kreiselpumpen der chemischen Industrie (1957)
    Weinheim : Wiley-Blackwell
    Chemie Ingenieur Technik - CIT 29 (1957), S. 241-249 
    Details
    ISSN: 0009-286X
    Keywords: Chemistry ; Industrial Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: Die Abdichtung der Wellendurchführung bei Kreiselpumpen für die chemische Industrie ist eine der wichtigsten Aufgaben des Pumpenkonstrukteurs. Die Gleitringdichtung wird immer mehr verwendet und wird in den verschiedensten Ausführungen hergestellt. An die Oberflächenglätte der beiden aufeinander gleitenden Dichtringe werden besondere Anforderungen gestellt. Die Unebenheiten an der gleitenden Oberfläche sollen unter 1 μ sein. Es wird versucht, die inneren Vorgänge der Druckentspannung zwischen den beiden Gleitringen zu erklären. Die Werkstoffe für Gleitringdichtungen, speziell für korrodierende Medien, werden besprochen, zulässige Drucke und Temperaturen werden angegeben.
    Additional Material: 21 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cite.330290403
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  • 8
    Electronic Resource
    Electronic Resource
    Fluidized-bed receptor-affinity chromatography (1994)
    New York, NY : Wiley-Blackwell
    Biomedical Chromatography 8 (1994), S. 236-241 
    Details
    ISSN: 0269-3879
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Medicine
    Notes: A multipurpose fluidized-bed receptor-affinity purification system based upon the biological recognition between an immobilized receptor and its soluble protein ligands is described. The fluidized affinity sorbent consists of a soluble form of interleukin-2 receptor chemically bonded to an aldehyde derivative of controlled pore glass beads, which have a pore diameter of 1000 Å and a particle density of 1.2-1.3 g/mL. The fluidized-bed separation device used in this study consists of a specially designed column fitted at the inlet end with a perforated distributor plate covered with a screen and the top outlet with an adjustable piston. The fluidized-bed consisting of a loose gel matrix permits the unimpeded passage of cell debris and particulate matter, while the target protein is captured by the affinity beads. Purification of the humanized-anti-Tac monoclonal antibody is used as a model system to determine the operational parameters. Also, fluidized-bed receptor-affinity chromatography has been successfully employed in the purification of recombinant interleukin-2 and single chain anti-Tac(Fv)-Pseudomonas exotoxin immunotoxin from unclarified inclusion body extracts. Overall, fluidized-bed receptor-affinity chromatography is found to be a productive affinity method suitable for the purification of recombinant human interleukin-2 and related molecules.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/bmc.1130080508
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  • 9
    Electronic Resource
    Electronic Resource
    Predicting structural effects in HIV-1 protease mutant complexes with flexible ligand docking and protein side-chain optimization (1998)
    New York, NY : Wiley-Blackwell
    Proteins: Structure, Function, and Genetics 33 (1998), S. 295-310 
    Details
    ISSN: 0887-3585
    Keywords: molecular recognition ; Monte Carlo docking ; dead-end-elimination ; rotamer library ; correlated energy landscapes ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Medicine
    Notes: We present a computational approach for predicting structures of ligand-protein complexes and analyzing binding energy landscapes that combines Monte Carlo simulated annealing technique to determine the ligand bound conformation with the dead-end elimination algorithm for side-chain optimization of the protein active site residues. Flexible ligand docking and optimization of mobile protein side-chains have been performed to predict structural effects in the V32I/I47V/V82I HIV-1 protease mutant bound with the SB203386 ligand and in the V82A HIV-1 protease mutant bound with the A77003 ligand. The computational structure predictions are consistent with the crystal structures of these ligand-protein complexes. The emerging relationships between ligand docking and side-chain optimization of the active site residues are rationalized based on the analysis of the ligand-protein binding energy landscape. Proteins 33:295-310, 1998. © 1998 Wiley-Liss, Inc.
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Correlation of hydrogen solubilities in nonpolar solvents based on scaled-particle theory (1981)
    Hoboken, NJ : Wiley-Blackwell
    AIChE Journal 27 (1981), S. 844-848 
    Details
    ISSN: 0001-1541
    Keywords: Chemistry ; Chemical Engineering
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Process Engineering, Biotechnology, Nutrition Technology
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/aic.690270522
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