Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities

作者：Faist Johanna; Seebacher Werner; Kaiser Marcel; Brun Reto; Saf Robert; Weis Robert^*

来源：European Journal of Medicinal Chemistry, 2010, 45(1): 179-185.

DOI：10.1016/j.ejmech.2009.09.040

• 5-Amino-2-azabicyclo[3.2.2]nonane derivatives
• In vitro assay
• Plasmodium falciparum
• Trypanosoma brucei rhodesiense

N-Alkyl and N-(2-dialkylaminoethyl) derivatives of 5-amino-2-azabicyclo-nonanes were prepared and tested in vitro for their activities against the multidrug-resistant K(1) strain of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). Most of the new compounds showed lower antitrypanosomal activity than their parent compounds. With respect to their activity against P. falciparum the N-alkyl derivatives exhibited worse selectivity due to decreased antiplasmodial activity or higher cytotoxicity. In comparison all of the new N-(2-dialkylaminoethyl) analogues possessed a much better selectivity and a single of these compounds showed even better antiplasmodial activity and selectivity than chloroquine.

• 出版日期2010-1