Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores.

与四唑或磺酰胺核心连接的氮杂双环壬烷的抗原生动物活性

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作者:Dolensky Johanna, Hinteregger Clemens, Leitner Andreas, Seebacher Werner, Saf Robert, Belaj Ferdinand, Mäser Pascal, Kaiser Marcel, Weis Robert
N-(Aminoalkyl)azabicyclo[3.2.2]nonanes possess antiplasmodial and antitrypanosomal activity. A series with terminal tetrazole or sulfonamido partial structure was prepared. The structures of all new compounds were confirmed by NMR and IR spectroscopy and by mass spectral data. A single crystal structure analysis enabled the distinction between isomers. The antiprotozoal activities were examined in vitro against strains of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). The most active sulfonamide and tetrazole derivates showed activities in the submicromolar range.

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