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  • 1
    Electronic Resource
    Electronic Resource
    Rational design of hirulog-type inhibitors of thrombin (1994)
    Springer
    Journal of computer aided molecular design 8 (1994), S. 479-490 
    Details
    ISSN: 1573-4951
    Keywords: Molecular structure-based inhibitor design ; Molecular mechanics and dynamics ; Bifunctional inhibitors ; Thrombin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary The two crystal structures of thrombin complexed with its most potent natural inhibitor hirudin and with the active-site inhibitor d-Phe-Pro-Arg-CH2Cl [Rydel, T.J. et al., J. Mol. Biol., 221 (1991) 583; Bode, W. et al., EMBO J., 8 (1989) 3467] were used as a basis to design a new inhibitor, combining the high specificity of the polypeptide hirudin with the simpler chemistry of an organic compound. In the new inhibitor, the C-terminal amino acid residues 53–65 of hirudin are linked by a spacer peptide of four glycines to the active-site inhibitor NAPAP (Nα-(2-naphthyl-sulfonyl-glycyl)-dl-p-amidinophenylalanyl-piperidine). Energy minimization techniques served as a tool to determine the preferred configuration at the amidinophenylalanine and the modified piperidine moiety of the inhibitor. The predictions are supported by the interaction energies determined for d- and l-NAPAP in complex with thrombin, which are in good agreement with experimentally determined dissociation constants. The conformational flexibility of the linker peptide in the new inhibitors was investigated with molecular dynamics techniques. A correlation between the P1′ position and the interactions of the linker peptide with the protein is suggested. Modifications of the linker peptide are proposed based on the distribution of its main-chain torsion angles in order to enhance its binding to thrombin.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00123661
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  • 2
    Electronic Resource
    Electronic Resource
    Mikrobiologische Umwandlungen nichtsteroider Strukturen, V. Mikrobiologische Reaktionen von substituierten 1-Äthyl-4-oxo-1,4-dihydrochinolin-3-carbonsäuren (1973)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 106 (1973), S. 2636-2642 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Microbiological Transformations of Nonsteroidal Structures, V. Microbiological Reactions of Substituted 1-Ethyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acids1-Ethyl-7-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (1) is transformed to the methyl ester by Streptomyces surinam. Penicillium adametzi hydroxylates the substrate at the 7-methyl substituent, whereas 1 -ethyl-8-methoxy-5-methyl-4-oxo- 1,4-dihydroquinoline-3-carboxylic acid (4) is hydrolyzed to the free phenol by the same fungi. l-Ethyl-4-oxo-1,4,6,7,8,9-hexahydrobenzo[g]quinolinc-3-carboxylic acid (6) is hydroxylated in 7 - and 8-position by Penicillium adametzi, in 6- and 7- (or 8-) position by Streptomyces achromogenes and in 6-position by Sporotrichum sulfurescens. 5-Ethyl-8-oxo-2,3,5,8-tetrahydrofuro[2,3-g]quinoline-7-carboxylic acid (10) undergoes only a hydrolytic cleavage of the dihydrofuranering.
    Notes: 1-Äthyl-7-methyl-4-oxo-1,4-dihydrochinolin-3-carbonsäure (1) wird durch Streptomyces surinam in den Methylester umgewandelt. Penicillium adametzi hydroxyliert das Substrat am 7-Methylsubstituenten, während bei der 1 -Äthyl-8-methoxy-5-methyl-4-oxo- 1, 4-dihydrochinolin-3-carbonsäure (4) mit dem gleichen Pilz nur eine Phenolätherspaltung eintritt. 1-Äthyl-4-oxo-l,4,6,7,8,9-hexahydrobenzo[g]chinolin-3-carbonsäure (6) wird von Penicillium adametzi in 7- und 8-, von Streptomyces achromogenes in 7-(oder 8-) und 6- sowie von Spororrichum sulfurescens in 6-Stellung hydroxyliert. 5-Äthyl-8-oxo-2,3,5,8-tetrahydrofuro[2,3-g]-chinolin-7-carbonsäure (10) zeigt nur eine hydrolytische Spaltung des Dihydrofuranringes.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19731060827
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  • 3
    Electronic Resource
    Electronic Resource
    Mikrobiologische Umwandlungen nichtsteroider Strukturen, VII. Mikrobielle Glucosidierung einer phenolischen Hydroxylgruppe (1976)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 109 (1976), S. 2259-2265 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Microbiological Transformations of Nonsteroidal Structures, VII. Microbiological Glucosidation of a Phenolic Hydroxyl Group5,7-Dichloro-2-methyl-8-quinolinol (1) is transformed to the 4-O-methyl-β-glucoside (2) by Sporotrichum sulfurescens (ATCC 7159). 5-Chloro-2-methyl-7,8-quinolinediol (3) yields the 7- and the 8-(4-O-methyl-β-glucoside) (4,5). 6-Hydroxytetralone forms also the 4-O-methyl-β-glucoside (7). Bis(4-acetoxyphenyl)methylenecyclohexane (8) is transformed after intermediary saponification to the mono-4O-methyl-β-glucoside (10) by Sporotrichum sulfurescens, whereas Rhizopus colinii (ATCC 8996) forms the unsubstituted mono-β-glucoside (11).
    Notes: 5,7-Dichlor-2-methyl-8-chinolinol (1) wird mit Sporotrichum sulfurescens (ATCC 7159) in das 4-O-Methyl-β-glucosid 2 übergeführt. 5-Chlor-2-methyl-7,8-chinolindiol (3) ergibt sowohl das 7-als auch das 8-(4-O-Methyl-β-glucosid) (4,5). 6-Hydroxytetralon (6) bildet ebenfalls ein 4-O-Methyl-β-glucosid (7). Bis(4-acetoxyphenyl)methylencyclohexan (8) wird nach intermediärer enzymatischer Verseifung mit Sporotrichum sulfurescens in ein Mono-4-O-methyl-β-glucosid (10) umgewandelt, während Rhizopus colinii (ATCC 8996) ein unsubstituiertes β-Glucosid (11) bildet.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19761090632
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  • 4
    Electronic Resource
    Electronic Resource
    Notiz zur Herstellung eine Pyrido [2.3-b]pyrazins durch Gould-Jacobs-Reaktion (1972)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 105 (1972), S. 3118-3120 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19721050935
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  • 5
    Electronic Resource
    Electronic Resource
    Synthese von 20-Oxo-Δ16-pregnenen durch Eliminierung der 17-Nitrooxygruppe (1974)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 107 (1974), S. 1235-1244 
    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 20-Oxo-Δ16-steroids by Elimination of the 17-Nitrooxy GroupThe hydroxysteroids 1a-f react with acetyl nitrate to yield the 11β,17-dinitrates 1h-k or the 17-nitrates 11-o, respectively. Treatment of the nitrate esters 1h-o with potassium acetate in dimethylformamide above 1007°C results in the formation of the Δ16-steroids 3h-o and 4 by elimination of the 17-nitrooxy group. When the reaction is carried out at temperatures below 80°C, the enol acetates 2a, h, i and 1, are isolated which can be transformed into the Δ16-compounds. From the 11β-nitrooxysteroids 3j and k there was obtained the 11β-hydroxy-Δ16-steroids 3n and d, respectively, by reaction with zinc dust.
    Notes: Die Hydroxysteroide 1a-f bilden mit Acetylnitrat die 11β.17-Dinitrate 1h-k bzw. die 17-Nitrate 11-o. Unter der Einwirkung von Kaliumacetat in Dimethylformamid entstehen aus 1h-o oberhalb von 100°C durch Abspaltung der 17-Nitrooxygruppe die Δ16-Steroide 3h-o und 4. Bei Reaktionstemperaturen unterhalb 80°C können die Enolacetate 2a, 2h, i und 1 isoliert werden, die sich in Δ16-Verbindungen überführen lassen. Aus den 11β-Nitro-oxysteroiden 3j und k werden durch Reaktion mit Zinkstaub in Eisessig die 11β-Hydroxy-Δ16-Verbindungen 3n bzw. d gebildet.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19741070420
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  • 6
    Electronic Resource
    Electronic Resource
    Eine ungewöhnliche Reaktion von Acetylendicarbonsäure-dimethylester mit 2-Amino-3-thiophencarbonsäure-ethylester (1978)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 111 (1978), S. 770-779 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: An Unusual Reaction of Dimethyl Acetylenedicarboxylate with Ethyl 2-Amino-3-thiophenecarboxylateEthyl 2-amino-3-thiophenecarboxylate (3) reacts with dimethyl acetylenedicarboxylate to give a multiple component mixture which does not only contain the expected Michael adduct 4 in modest yield, but the cyclo-adducts 5, 6, and 7, too. The structures of these products are determined and the mechanism of their formation is discussed.
    Notes: 2-Amino-3-thiophencarbonsäure-ethylester (3) reagiert mit Acetylendicarbonsäure-dimethylester zu einem Mehrkomponentengemisch, das neben dem erwarteten Michael-Addukt 4 noch die Cycloaddukte 5, 6 und 7 enthält. Die Konstitution dieser Produkte wird ermittelt und ihre Bildung diskutiert.
    Additional Material: 3 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19781110236
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  • 7
    Electronic Resource
    Electronic Resource
    Mikrobiologische Umwandlung von Steroiden, XVI. Synthese von 11β, 21-Dihydroxy-6, 16α-dimethyl-1,4,6,-pregnatrien-3,20-dion und dessen 11-Ketoverbindung (1979)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 112 (1979), S. 979-989 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Microbial Transformations of Steroids XVI. Synthesis of 11β,21-Dihydroxy-6, 16α-dimethyl-1,4,6-pregnatriene-3,20-dione and of its 11-Keto Compound21-Acetoxy-5α,6α-epoxy-3β-hydroxy-6β16α-dimethyl-20-pregnanone (3a), prepared from 3β-hydroxy-6, 16α-dimethyl-5-pregnen-20-one (1) by epoxidation and chemical introduction of the 21-acetoxy group, was oxidized to 6α,21-dihydroxy-6β,16α-dimethyl-4-pregnene-3,20-dione (4) by Flavobacterium dehydrogenans and dehydrated to the 3-keto-4,6-diene 5. The 11β-hydroxy group was introduced by Curvularia lunata to give 6, and the 11α-hydroxy group by Aspergillus ochraceus to yield 8. Both compounds were dehydrogenated with Bacillus lentus to from 7 and 9. The 11α-hydroxy compound 9 was selectively acetylated to 10, which was oxidize to 11. This on saponification yielded 12.
    Notes: 21-Acetoxy-5α,6α-epoxy-3β-hydroxy-6β,16α-dimethyl-20-pregnanon (3a), dargestellt aus 3β-Hydroxy-6, 16α-dimethyl-5-pregnen-20-on (1) durch Epoxidierung und 21-Acetoxylierung, wurde mit Flavobacterium dehydrogenans zu 6α,21-Dihydroxy-6β, 16α, -dimethyl-4-pregnen-3,20-dion (4) oxidiert und zu 21-Hydroxy-6, 16α-dimethyl-4,6-pregnadien-3,20-dion (5) dehydratisiert. Mit Curvularia lunata wurde die 11β-Hydroxygruppe eingeführt zu 6, während Aspergillus ochraceus die entsprechende 11α-Hydroxyverbindung 8 ergab. Beide Verbindungen wurden mit Bacillus lentus zu 7 bzw. 9 dehydriert. Die 11α-Hydroxyverbindung 9 wurde nach selektiver Acetylierung der 21-Hydroxygruppe zu 10 zum 11-Keton 11 oxidiert, dessen Verseifung 12 ergab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19791120320
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  • 8
    Electronic Resource
    Electronic Resource
    Mikrobiologische Umwandlung von Steroiden, XVII. Darstellung von unterschiedlichen Mono- und Diketostrukturen von D-Homo-4-pregnen-3,20-dion und D-Homo-1,4-pregnadien-3,20-dion (1980)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 113 (1980), S. 203-220 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Microbial Transformations of Steroids, XVII. Preparation of Several Mono- and Diketo-structures of D-Homo-4-pregnene-3,20-dione and D-Homo-1,4-pregnadiene-3,20-dione11α- (2) and 15α-monohydroxy- (3), 6β,11α-(4), 11α,15α- (5), 12β,15α- (6), 15α,16α- (7), 7β,11α- (8), 11β,17α- (9), 7β,17α-dihydroxy- (11), and 17α-hydroxy-11-oxo-D-homoprogesterone (10) were prepared by microbiological transformations of D-homoprogesterone (1) with various fungi. The compounds were oxidized by the method of Jones before and after microbiological 1,2-dehydrogenation with Bacillus lentus to the corresponding keto-structures 12 to 17 and 20 respectively 26 to 30. The 14α-hydroxy-11-ketone 18 and 7α,14α-dihydroxy-11-ketone 19 were obtained by microbiological hydroxylation of the 11-ketone 12 with Curvularia lunata. Penicillium lilacinum degraded D-homoprogesterone (1) to D-homotestosterone.
    Notes: Durch mikrobiologische Umwandlung von D-Homoprogesteron (1) mit verschiedenen Pilzstämmen wurden 11α- (2) und 15α-Monohydroxy- (3), 6β,11α- (4), 11α,15α- (5), 12β,15α- (6), 15α,16α- (7), 7β,11α- (8), 11β,17α- (9), 7β,17α-Dihydroxy- (11) und 17α-Hydroxy-11-oxo-D-homo-progesteron (10) hergestellt. Die Verbindungen wurden vor und nach mikrobiologischer 1,2-Dehydrierung mit Bacillus lentus zu den entsprechenden Ketostrukturen 12 - 17 und 20 bzw. 26 - 30 nach Jones oxidiert. Ein 14α-Hydroxy-11-keton 18 und 7α,14α-Dihydroxy-11-keton 19 wurden durch mikrobiologische Zweithydroxylierung des 11-Ketons 12 mit Curvularia lunata erhalten. Penicillium lilacinum baute D-Homoprogesteron (1) zu D-Homotestosteron ab.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19801130121
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  • 9
    Electronic Resource
    Electronic Resource
    Mikrobiologische Umwandlungen nichtsteroider Strukturen, IV. Mikrobiologische Spaltung eines Nitrofuran-Derivates (1973)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 106 (1973), S. 1303-1308 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Microbiological Transformations of Nonsteroidal Structures, IV. Microbiological Cleavage of a Nitrofurane Derivative5-Methoxy-2-(5-nitrofurfurylidene)-1-indanone (1) is opened by several microorganisms reductively to yield 2-(4-cyano-2-oxobutyl)-5-methoxy-1-indanone (2). In part an additional cleavage of the phenolic methoxy group occurs with formation of 2-(4-cyano-2-oxobutyl)-5-hydroxy-1-indanone (3).
    Notes: 5-Methoxy-2-(5-nitrofurfuryliden)-1-indanon (1) wird von mehreren Mikroorganismen reduktiv zu 2-(4-Cyan-2-oxobutyl)-5-methoxy-1-indanon (2) geöffnet. Teilweise erfolgt zusätzlich eine Spaltung der phenolischen Methyläthergruppe zu 2-(4-Cyan-2-oxobutyl)-5-hydroxy-1-indanon (3).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19731060427
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  • 10
    Electronic Resource
    Electronic Resource
    Mikrobiologische Umwandlungen nichtsteroider Strukturen, VIII: Mikrobiologische Umwandlungen von (±)-8-Hydroxy-6α, 11α-dimethyl-3-alkyl-oder-3-acyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocinen (1976)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 109 (1976), S. 2657-2669 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Microbiological Transformations of Nonsteroidal structures, VIII: Microbiological Transformations of (±)-8-Hydroxy-6α, 11α-dimethyl-3-alkyl-or-3-acyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocins±-8-Hydroxy-6α, 11α-dimethyl-3-(3-methylbutyl)1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin (1) is transformed microbiologically to the 3′-hydroxy-compound (2). The N-benzoate of the corresponding 3-desalkyl-compound is hydroxylated by several fungi in 1α-position (9). The hydroxylation of the 4- and 4′-position (11, 12), the oxidation to a 3- (3,4-epoxy-1,5-cyclohexadiene-carbonyl) structure (13) and the formation of a 8-pentosyl glycoside (10) are sidereactions. The fermentation of the N-cyclohexylcarbonyl derivative (14) leads to hydroxylations of the cyclohexylring in the axial 3′-and 4′(15 and 17) and in the euqatorial 4′ -position (16).
    Notes: ±-8-Hydroxy-6α, 11α-dimethyl-3-(3-methylbutyl)-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin (1) wird mikrobiologisch zur 3′-Hydroxyverbindung (2) umgewandelt. Das N-Benzoylderivat (8) der entsprechenden 3-Desalkylverbindung wird durch unterschiedliche Fungi in 1α-Stellung (9) hydroxyliert. Die Hydroxylierung der 4- und 4′-Stellung (11,12), die Oxidation zu einer 3-(3,4-Epoxy-1,7-cyclohexadiencarbonyl)-struktur (13) und die Bildung eines 8-Pentosylglycosids (10) treten als Nebenreaktionen auf. Bei der Fermentation des N-Cyclohexylcarbonyl-Derivates (14) entstehen Hydroxylierungsprodukte des Cyclohexylrestes in den axialen 3′- und 4′-Positionen (15 und 17) und in der äquatorialen 4′-Position (16).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19761090802
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