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KMID : 0043320080310060688
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Archives of Pharmacal Research
2008 Volume.31 No. 6 p.688 ~ p.697
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Synthesis of Bicyclic Amines and Their Activities Against Trypanosoma brucei rhodesiense and Plasmodium falciparum K₁
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Weis Robert
Berger Heinrich
Kaiser Marcel
Brun Reto
Saf Robert
Seebacher Werner
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Abstract
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New alkenes, aziridines, and diamines were prepared from antiprotozoal 4-dialkylaminobicyclo[2.2.2]octan-2-imines to investigate the influence of several functional groups in position 2 of the ring skeleton on the antitrypanosomal and antiplasmodial activities. They were synthesized from 4-dialkylaminobicyclo[2.2.2]octan-2-imines and tested for their activities against Trypanosoma b. rhodesiense and Plasmodium falciparum (resistant to chloroquine and pyrimethamine) using in vitro microplate assays. 4-Aminobicyclo[2.2.2]oct-2-enes and 3-azatricyclo[]nonylamines exhibit similar antiprotozoal activities as 4-aminobicyclo[2.2.2] octanes. 4-Aminobicyclo[2.2.2]oct-2-ylamines and their N-benzyl derivatives showed decreased antiplasmodial but enhanced antitrypanosomal () activities compared to their parent oximes and to formerly synthesized 4-amino-2-azabicyclo[3.2.2]nonanes. Some of the 4-aminobicyclo[2.2.2]oct-2-ylamines exhibit moderate in vivo activity in mice against Trypanosoma brucei brucei.
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KEYWORD
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4-Dialkylaminobicyclo[2.2.2]octane derivatives, Bicyclic diamines, Antiplasmodial activity, Antitrypanosomal activity, In vitro microplate assays
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