9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma
| العنوان: | 9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma |
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| المؤلفون: | Mahin Abad Dar, Franziska Maiwald, Diego Benítez, Laurent Meijer, Nadège Loaëc, Conrad Kunick, Lutz Preu, Hanna Erdmann, Marcelo A. Comini, Oliver Koch, Diego Charquero, Christoph Hölscher |
| المساهمون: | Technische Universität Braunschweig = Technical University of Braunschweig [Braunschweig], Institut Pasteur de Montevideo, Réseau International des Instituts Pasteur (RIIP), Forschungszentrum Borstel - Research Center Borstel, Technische Universität Dortmund [Dortmund] (TU), ManRos Therapeutics, This project was funded by the German 'Bundesministerium für Bildung und Forschung' (KMU-innovativ 5, Förderkennzeichen 0315814, to F. M., M. A. D., O. K., C. H., and C. K.). The support of FOCEM (MERCOSUR Structural Convergence Fund, COF 03/11) and ANII (grant Innova Uruguay, agreement DCI-ALA/2007/19.040 between Uruguay and the European Commission, INI_X_2011_1_4077 and POS_NAC_2013_1_114477) is acknowledged by M. A. C., D. B. and D. C.. L. M. was supported by a grant from the ‘Agence Nationale de la Recherche’ (ANR- 11-RPIB-0016 grant, Transleish). |
| المصدر: | European Journal of Medicinal Chemistry European Journal of Medicinal Chemistry, Elsevier, 2014, 83, pp.274-283. ⟨10.1016/j.ejmech.2014.06.020⟩ |
| بيانات النشر: | Elsevier BV, 2014. |
| سنة النشر: | 2014 |
| مصطلحات موضوعية: | MESH: Trypanocidal Agents/chemical synthesis, MESH: Benzazepines/toxicity, Nagana, Mice, Chalcones, MESH: Structure-Activity Relationship, MESH: Cell Proliferation/drug effects, Human trypanosomiasis, Drug Discovery, MESH: Animals, MESH: Benzazepines/chemistry, biology, MESH: Trypanosoma brucei brucei/physiology, Chemistry, MESH: Macrophages/drug effects, General Medicine, Trypanocidal Agents, 3. Good health, MESH: Trypanocidal Agents/pharmacology, Biochemistry, Paullones, MESH: Trypanocidal Agents/toxicity, MESH: Trypanosomiasis, African/parasitology, Trypanosoma brucei brucei, Cell Line, Structure-Activity Relationship, Heck reaction, parasitic diseases, medicine, Animals, Humans, [SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology, MESH: Trypanosoma brucei brucei/drug effects, MESH: Drug Design, MESH: Mice, Cell Proliferation, Pharmacology, MESH: Humans, MESH: Benzazepines/chemical synthesis, MESH: Trypanocidal Agents/chemistry, Macrophages, Organic Chemistry, MESH: Benzazepines/pharmacology, Benzazepines, biology.organism_classification, medicine.disease, Antiparasitic agent, Cinnamides, MESH: Cell Line, Trypanosomiasis, African, Drug Design, Trypanosoma |
| الوصف: | International audience; Trypanosomes from the "brucei" complex are pathogenic parasites endemic in sub-Saharan Africa and causative agents of severe diseases in humans and livestock. In order to identify new antitrypanosomal chemotypes against African trypanosomes, 4-azapaullones carrying α,β-unsaturated carbonyl chains in 9- or 11-position were synthesized employing a procedure with a Heck reaction as key step. Among the so prepared compounds, 5a and 5e proved to be potent antiparasitic agents with antitrypanosomal activity in the submicromolar range. |
| تدمد: | 0223-5234 1768-3254 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0f950885441e6cd8f086d1dfed0feca https://doi.org/10.1016/j.ejmech.2014.06.020 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....f0f950885441e6cd8f086d1dfed0feca |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 02235234 17683254 |
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