Novel Azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense
| Autor: | Heinrich Berger, Marcel Kaiser, Werner Seebacher, Robert Weis, Reto Brun, Robert Saf |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
medicine.drug_class
Stereochemistry Plasmodium falciparum Trypanosoma brucei brucei Clinical Biochemistry Pharmaceutical Science Carboxamide Trypanosoma brucei Biochemistry Chemical synthesis Antimalarials chemistry.chemical_compound parasitic diseases Drug Discovery medicine Animals Molecular Biology biology Bicyclic molecule Chemistry Aryl Organic Chemistry Trypanosoma brucei rhodesiense biology.organism_classification Trypanocidal Agents Antiprotozoal Molecular Medicine Azabicyclo Compounds |
| Zdroj: | Bioorganic & Medicinal Chemistry. 16:6371-6378 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2008.05.007 |
| Popis: | New diaryl substituted 2-azabicyclo[3.2.2]nonane derivatives have been synthesized in order to investigate the influence of the aromatic substitution and of N substitution on the antiprotozoal activities of those compounds. Following a manual method for the Hansch approach, different 4-substituted aryl rings were systematically inserted, and moieties with varying basicity and polarity were attached to the ring nitrogen. All compounds were investigated for their activities against Trypanosoma brucei rhodesiense (STIB 900) and the K 1 strain of Plasmodium falciparum (resistant to chloroquine and pyrimethamine) and for their cytotoxicity using microplate assays. Some of the new compounds are amongst the most active antitrypanosomal agents in this series, and the selectivity index of a single derivative is superior in the 2-azabicyclo-nonane series. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect