Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals Original Research Article

A couple of bicyclo[2.2.2]octyl esters of 2-dialkylaminoacetic acids were prepared. Their antiplasmodial and antitrypanosomal activities against Trypanosoma brucei rhodesiense (STIB 900) and the K1 strain of Plasmodium falciparum (resistant to chloroquine and pyrimethamine) were determined using microplate assays. Structure–activity relationships were discussed. The antiprotozoal activities were remarkably increased by insertion of a second basic centre. The selectivity indices of the most active compounds are superior in the bicyclo-octane series.