Antimalarial in-vivo activity of bis(9-amino-6-chloro-2-methoxyacridines)
| Autor: | Amaya Berecibar, Philippe Grellier, Christian Sergheraert, Pascal Lemiere, Louis Maes, L. Quirijnen, Sandrine Delarue, Sophie Girault, Marie-Ange Debreu-Fontaine |
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| Rok vydání: | 2001 |
| Předmět: |
Pharmacology
Aminoacridines Plasmodium berghei Stereochemistry Pharmaceutical Science Chloroquine Biological activity Biology biology.organism_classification Chemical synthesis In vitro Malaria Antimalarials Mice chemistry.chemical_compound chemistry Biochemistry In vivo Toxicity Acridine Animals Female Polyamine |
| Zdroj: | Journal of Pharmacy and Pharmacology. 53:935-938 |
| ISSN: | 2042-7158 0022-3573 |
| DOI: | 10.1211/0022357011776333 |
| Popis: | In the fight against malaria, chemotherapy using bisacridines may represent an alternative method to overcoming chloroquine-resistance. Eight bis(9-amino-6-chloro-2-methoxyacri-dines), in which acridine moieties were linked by polyamines substituted with a side chain, were tested for their in-vivo activity upon mice infected by Plasmodium berghei. Three of the compounds revealed antimalarial activity but no relationship could be deduced from a comparison of in-vitro and in-vivo activities. N-alkylation of the central amino group generated toxicity and, therefore, only compounds N-acylated in this position can be selected as leads. |
| Databáze: | OpenAIRE |
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