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  • 1
    Book
    Book
    Stuttgart : Wiss. Verl.-Ges.
    Keywords: Arzneimittel ; Stereochemie ; Arzneimittel ; Stereochemie
    Type of Medium: Book
    Pages: 324 S. , Ill., graph. Darst.
    ISBN: 3804714854
    RVK:
    Language: German
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  • 2
    Book
    Book
    Stuttgart : Dt. Apotheker-Verl.
    Keywords: Chemistry, Pharmaceutical ; Pharmakologie ; Klinische Chemie ; Pharmazeutische Chemie ; Lehrbuch ; Pharmakologie ; Klinische Chemie ; Pharmazeutische Chemie
    Type of Medium: Book
    Pages: XVI, 703 S. , Ill., graph. Darst.
    Edition: 2., völlig neu bearb. und erw. Aufl.
    ISBN: 9783769250022
    DDC: 615.1
    RVK:
    RVK:
    Language: German
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  • 3
    Book
    Book
    Stuttgart : Wissenschaftliche Verl.ges.
    Keywords: Pharmazie ; Taschenbuch ; Pharmazie ; Taschenbuch
    Type of Medium: Book
    Pages: Lfgs.-Werk
    Edition: 10. Aufl.
    ISBN: 3804712789
    RVK:
    Language: Undetermined
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 3 (1986), S. 271-277 
    ISSN: 1573-904X
    Keywords: leukotriene B4 ; 5-lipoxygenase ; chemiluminescence ; pyrrolopyrimidines ; pyrrol derivatives ; polymorphonuclear granulocyte (PMNL) activation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The effect of several series of compounds on the biosynthesis of leukotriene B4 in human polymorphonuclear granulocytes (PMNL) was measured after stimulation of the cells by the Ca2+ ionophore A23187. Phenylhydrazone derivatives and some pyrrole derivatives strongly inhibited 5-lipoxygenase activity at 10 µM. In contrast, 4-aminopyrrolopyrimidines and 4-oxopyrrolopyrimidmes did not exhibit any effect. The compounds examined for inhibition of 5-lipoxygenase were also tested in a chemiluminescence assay for potential effects on the emission of photons as a measure of activated oxygen species generated by the stimulated granulocytes. There was a good correlation between lipoxygenase inhibition and suppression of chemiluminescence; however, some derivatives with no inhibitory activity against lipoxygenase still reduced chemiluminescence, which suggests that an alternative inhibitory mechanism of chemiluminescence must be present. Cyclooxygenase inhibitors such as aspirin did not suppress chemiluminescence of granulocytes. It is, therefore, unlikely that cyclooxygenase is required in the chemiluminescence reaction. In contrast, LTB4 seems to play an important role in the zymosan-induced chemiluminescence of PMNL.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Journal of molecular modeling 3 (1997), S. 332-337 
    ISSN: 0948-5023
    Keywords: Keywords: Dapsone ; Sulfonamides ; Mycobacterium leprae ; Lipophilicity ; Molecular Modeling
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Despite the very close structural relationship between dapsone (4,4′-diaminodiphenyl sulfone, 4,4′ sulphonyldianiline, diaphenyl sulphone, DDS) and sulfanilamide (p-aminobenzene sulfonamide), being the prototype of all other sulfonamides, only dapsone shows remarkable efficient pharmacological activity against Mycobacterium leprae. Cells of certain micro-organism need para-aminobenzoic acid (PABA), the latter playing the role of natural substrate to biosynthesis of folic acid. Sufones and sulfonamides show competitive antagonism as chemical analogs of PABA. It is most surprising that, despite of sharing this molecular mechanism, only dapsone shows anti-leprosy activity in vivo. The study was accomplished using molecular mechanics (SYBYL) and semiempirical methods (MOPAC). The calculations of aromaticity, charges, protonation by MOPAC, and of lipophilicity by our empirical program LIPOP(hilicity) give evidence that dapsone is more lipophilic (log P values 0.97) than sulfanilamide (-0.67). The extremely lipophilic cell wall of Mycobacterium leprae contributes to the surprising difference in anti-leprosy activity. Sulfonamides are more or less deprotonated (45 to 99 %) at physiological pH units, whereas dapsone is totally undissociated. This results in different permeability rates into the bacterial cells in vivo. Compared to other sulfones and sulfonamides, the unique combination of high lipophilicity and low ionic dissociation favors anti-leprotic potency in dapsone. On principle, amide groups do not hinder activity, but cause acidity and subsequently dissociation.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    ISSN: 1618-2650
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary Disaccharide fragments resulting from the enzymatic digestion of heparins with heparinase have been purified by gel filtration chromatography and directly analyzed by positive and negative ion liquid secondary ion mass spectrometry (LSIMS). Following the chromatographic purification from excess sodium salt, the mass spectra of di- and tetrasaccharide fragment mixtures enabled the identification of up to three covalently bound sulfate moieties per glycosaminoglycan-disaccharide unit, by means of their molecular ions, containing the corresponding alkali-counterions.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    ISSN: 1618-2650
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Modified calixarenes can be used as model compounds to study molecular recognition since their molecular cavities reversibly incorporate small organic molecules. This effect has been used in chemical sensors with bulk and surface acoustic wave devices, coated with thin calixarene layers. These devices sensitively convert the mass changes during molecule/calixarene interactions into electronic signals. Thin films of modified calixarenes were prepared with various side groups and various sizes by Knudsen sublimation under well-defined, ultra-high-vacuum conditions. The interaction with perchloroethylene, chloroform, benzene, and toluene at constant temperatures, T, and partial pressures, pi, was studied systematically for different film thicknesses, d, by means of mass changes Δm=f(T,p i,d). From the thickness dependence of values, Δmeq, obtained under thermodynamic equilibrium conditions, surface and bulk effects during molecule calixarene interactions were separated. Pronounced excesses of surface concentrations of organic molecules have been found. Activation energies for molecular desorption from surface sites and for diffusion to subsurface sites were determined from mass spectroscopic results of thermal desorption behaviour. Experimental data of adsorption and desorption energies were confirmed by theoretical force field calculations.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1986 (1986), S. 1485-1505 
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis of 7-Unsubstituted 7H-Pyrrolo[2,3-d]pyrimidinesThe title compounds 4 are obtained by N-7 dealkylation of the 2-furanylmethyl, 2-thio-phenylmethyl, or 1-phenylethyl group from 2a - g and 10 - j with polyphosphoric acid. In contrast to the 2-furanylmethyl group the 2-thiophenylmethyl and 1-phenylethyl group can be removed independently of the substitution of the heterobicycle.
    Notes: Die Titelverbindungen 4 werden durch N-7-Dealkylierung der 2-Furanylmethyl-, 2-Thiophenylmethyl-, oder 1-Phenylethyl-Gruppe aus den Derivaten 2a - g und 10a - j mit Polyphosphoräure erhalten. Im Gegensatz zur 2-Furanylmethyl-Gruppe lassen sich die 2-Thiophenylmethyl- und 1-Phenylethyl-Gruppen unabhängig von der Substitution am Heterobicyclus entfernen.
    Additional Material: 3 Tab.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1989 (1989), S. 51-57 
    ISSN: 0170-2041
    Keywords: Amphiphiles, chiral ; Liposomes ; s-Triazine ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis of Chiral Liposome Building Blocks with s-Triazine as Linking Unit1)In order to synthesize a variable system of well-defined one- and two-chain chiral amphiphiles that are able to form liposomes, we choose s-triazine as linking unit between the lipophilic and hydrophilic moieties. The lipophilic part is made of long-chain alcohols or alkylamines, whereas the hydrophilic part of the molecules is formed by the trifunctional amino acids L-cysteine, L-serine, or L-lysine. These are linked to the s-triazine with their ω-functional group. Because of the amino acid structure of the new lipids it is possible to examine their optical purity by thin-layer chromatography. On the investigation of their liposome-building properties only the cysteine amphiphiles with two alkyl chains are found to be capable of forming vesicles.
    Notes: Um ein variables System ein- und zweikettiger chiraler Amphiphile zu synthetisieren, die sich als Liposomenbausteine eignen, wurde s-Triazin als Verknüpfungseinheit zwischen lipophilem und hydrophilem Molekülteil ausgewählt. Der lipophile Teil besteht aus langkettigen Alkoholen oder Alkylaminen, während der hydrophile Teil der Moleküle durch die trifunktionellen Aminosäuren L-Cystein, L-Serin oder L-Lysin gebildet wird. Diese sind über ihre ω-Funktion mit dem s-Triazin verbunden. Aufgrund der Aminosäurestruktur der neuen Lipide ist eine dünnschichtchromatographische Kontrolle ihrer optischen Reinheit möglich. Bei der Untersuchung der neuen Verbindungen auf ihre Eignung als Vesikelbausteine erweisen sich nur die zweikettigen Cystein-Amphiphile als Liposomenbildner.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1989 (1989), S. 127-131 
    ISSN: 0170-2041
    Keywords: Amphiphiles, chiral ; Differential scanning calorimetry ; Fluorescence anisotropy ; Liposomes ; s-Triazines ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis and Aggregation Behaviour of Chiral Cysteine Amphiphiles with s-Triazine as Connecting UnitSeveral homologous liposome building blocks 3 with L-cysteine as chiral hydrophilic head group are synthesized. s-Triazine serves as connecting unit between cysteine and the lipophilic alkyl chains. The phase transition temperatures of the lipids are determined by DSC or fluorescence anisotropy. It can be shown, that the relationship between nature and length of the chains and the phase transition temperature corresponds to that of phospholipids. Encapsulation experiments with ionic water-soluble dyes give some hints that the vesicles prepared in phosphate buffer (pH = 7.0) interact with cationic but not with anionic hydrophilic substances.
    Notes: Es werden homologe Liposomenbausteine 3 mit L-Cystein als chirale hydrophile Kopfgruppe synthetisiert. Als Verknüpfungseinheit zwischen Cystein und den lipophilen Alkylketten dient s-Triazin. Mittels DSC- und Fluoreszenz-Anisotropie-Messungen lassen sich die Phasenübergangstemperaturen der Lipide bestimmen. Es kann gezeigt werden, daß eine den Phospholipiden analoge Relation zwischen Art und Länge der Ketten und der Phasenübergangstemperatur besteht. Einschlußversuche mit ionischen wasserlöslichen Farbstoffen ergeben Hinweise auf eine Interaktion der in Phosphatpuffer (pH = 7.0), gebildeten Vesikel mit kationischen, nicht jedoch mit anionischen hydrophilen Substanzen.
    Additional Material: 7 Tab.
    Type of Medium: Electronic Resource
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