Bioorganic & medicinal chemistry letters · 2015
Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.
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Seebacher Werner, Wolkinger Volker, Faist Johanna, Kaiser Marcel, Brun Reto, Saf Robert, Bucar Franz, Gröblacher Barbara, Brantner Adelheid, Merino Virginia, Kalia Yogeshvar, Scapozza Leonardo, Perozzo Remo, Weis Robert
Аннотация
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.
Предметные рубрики MeSH
Administration, OralAnimalsAntiprotozoal AgentsAzabicyclo CompoundsDisease Models, AnimalDose-Response Relationship, DrugInjections, IntravenousMaleMiceMolecular StructureParasitic Sensitivity TestsPlasmodium bergheiPlasmodium falciparumRatsStructure-Activity RelationshipTissue DistributionTrypanosoma brucei rhodesienseTrypanosomiasis, African