The bisnaphthalimides as new active lead compounds against Plasmodium falciparum
| Autor: | Maximilian Tischer, Gabriele Pradel, Ludmilla Sologub, Ulrike Holzgrabe |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Plasmodium falciparum Pharmaceutical Science Biochemistry Chemical synthesis Phosphatidylcholine Biosynthesis Cell Line chemistry.chemical_compound Antimalarials Structure-Activity Relationship Drug Discovery Animals Methylene Imide Cytotoxicity Molecular Biology biology Molecular Structure Chemistry Macrophages Organic Chemistry biology.organism_classification Naphthalimides Quaternary Ammonium Compounds Molecular Medicine Aliphatic compound |
| Zdroj: | Bioorganicmedicinal chemistry. 18(9) |
| ISSN: | 1464-3391 |
| Popis: | The bisquaternary bisnaphthalimides are a versatile class of compounds being active against the malaria parasite Plasmodium falciparum in the lower nanomolar range of concentration combined with no cytotoxicity. The series of compounds is designed as choline analogues and interfering agents of the phosphatidylcholine biosynthesis. The qualitative analysis of the structure-activity relationships (SAR) revealed the importance of a long methylene middle chain of at least 8 methylene groups between the two bisquaternary naphthalimides or a monoquaternary naphthalimide consisting of a long alkyl chain attached to the positively charged nitrogen atom. Since the SARs are different from reported biscationic antimalarial drugs the mode of action remains to be elucidated. |
| Databáze: | OpenAIRE |
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