6533b7cffe1ef96bd1258508

RESEARCH PRODUCT

Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.

Leonardo ScapozzaMarcel KaiserRemo PerozzoAdelheid BrantnerWerner SeebacherVolker WolkingerRobert SafRobert WeisJohanna FaistYogeshvar N. KaliaBarbara GröblacherReto BrunFranz BucarVirginia Merino

subject

MaleTrypanosoma brucei rhodesiensemedicine.drug_classPlasmodium bergheiClinical BiochemistryPlasmodium falciparumAntiprotozoal AgentsPharmaceutical ScienceAdministration OralBiochemistryMiceStructure-Activity RelationshipParasitic Sensitivity TestsChloroquineparasitic diseasesDrug DiscoverymedicineAnimalsPlasmodium bergheiTissue DistributionMolecular BiologyPathogenbiologyBicyclic moleculeDose-Response Relationship DrugMolecular StructureChemistryOrganic ChemistryPlasmodium falciparumTrypanosoma brucei rhodesiensebiology.organism_classificationRatsDisease Models AnimalPyrimethamineTrypanosomiasis AfricanBiochemistryInjections IntravenousAntiprotozoalMolecular MedicineAzabicyclo Compoundsmedicine.drug

description

Several bicyclic compounds, 3-azabicyclo[3.2.2]nonanes, have been prepared. The new compounds were tested for their activities against one strain of the causative organism of Malaria tropica, Plasmodium falciparum K1, which is resistant against chloroquine and pyrimethamine. In addition, their cytotoxicity and their activity against the pathogen of the East African form of sleeping sickness, Trypanosoma brucei rhodesiense, were investigated. Structure-activity relationships are discussed considering data of readily prepared compounds. For the first time, a distinct in vivo activity was observed against Plasmodium berghei in a mouse model. The active compound was further investigated.

yearjournalcountryeditionlanguage
2015-01-22Bioorganicmedicinal chemistry letters
10.1016/j.bmcl.2015.02.044https://pubmed.ncbi.nlm.nih.gov/25746816