| |  Online-Ressource |
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| Verfasst von: | Marcu, Ana [VerfasserIn]  |
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| | Schurigt, Uta [VerfasserIn] |
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| | Müller, Klaus [VerfasserIn] |
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| | Moll, Heidrun [VerfasserIn] |
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| | Krauth-Siegel, Renate [VerfasserIn] |
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| | Prinz, Helge [VerfasserIn] |
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| Titel: | Inhibitory effect of phenothiazine- and phenoxazine-derived chloroacetamides on leishmania major growth and trypanosoma brucei trypanothione reductase |
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| Verf.angabe: | Ana Marcu, Uta Schurigt, Klaus Müller, Heidrun Moll, R. Luise Krauth-Siegel, Helge Prinz |
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| E-Jahr: | 2016 |
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| Jahr: | 27 January 2016 |
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| Jahr des Originals: | 2015 |
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| Umfang: | 8 S. |
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| Fussnoten: | Available online 23 November 2015 ; Gesehen am 07.05.2020 |
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| Titel Quelle: | Enthalten in: European journal of medicinal chemistry |
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| Ort Quelle: | Amsterdam [u.a.] : Elsevier Science, 1987 |
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| Jahr Quelle: | 2016 |
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| Band/Heft Quelle: | 108(2016), Seite 436-443 |
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| ISSN Quelle: | 1768-3254 |
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| Abstract: | A number of phenothiazine-, phenoxazine- and related tricyclics-derived chloroacetamides were synthesized and evaluated in vitro for antiprotozoal activities against Leishmania major (L. major) promastigotes. Several analogs were remarkably potent inhibitors, with antileishmanial activities being comparable or superior to those of the reference antiprotozoal drugs. Furthermore, we explored the structure-activity relationships of N-10 haloacetamides that influence the potency of such analogs toward inhibition of L. major promastigote growth in vitro. With respect to the mechanism of action, selected compounds were evaluated for time-dependent inactivation of Trypanosoma brucei trypanothione reductase. Our results are indicative of a covalent interaction which could account for potent antiprotozoal activities. |
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| DOI: | doi:10.1016/j.ejmech.2015.11.023 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: http://dx.doi.org/10.1016/j.ejmech.2015.11.023 |
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| | DOI: https://doi.org/10.1016/j.ejmech.2015.11.023 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | Acetamides |
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| | Antileishmanial activity |
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| | Antiprotozoal Agents |
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| | Chloroacetamides |
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| | Dose-Response Relationship, Drug |
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| | Enzyme Inhibitors |
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| | Leishmania major |
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| | Molecular Structure |
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| | NADH, NADPH Oxidoreductases |
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| | Oxazines |
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| | Parasitic Sensitivity Tests |
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| | Phenothiazines |
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| | Phenoxazines |
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| | Structure-Activity Relationship |
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| | Trypanosoma brucei brucei |
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| | Trypanothione reductase |
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| K10plus-PPN: | 1697697682 |
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| Verknüpfungen: | → Zeitschrift |
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Inhibitory effect of phenothiazine- and phenoxazine-derived chloroacetamides on leishmania major growth and trypanosoma brucei trypanothione reductase / Marcu, Ana [VerfasserIn]; 27 January 2016 (Online-Ressource)
