New derivatives of bicyclic diamines with antiprotozoal activity

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

来源：Monatshefte fur Chemie, 2016, 147(2): 369-381.

DOI：10.1007/s00706-015-1592-7

• Amines
• Carbonyl compounds
• Nucleophilic substitutions
• Antiplasmodial activity

omega-Aminoacyl and -alkyl derivatives of 4-(dialkylamino)bicyclo[2.2.2]octan-2-amines and of 5-(dialkylamino)-2-azabicyclo[3.2.2]nonanes were prepared and their activities were examined in vitro against the multiresistant K-1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). The results of the biological tests of the newly synthesized compounds were compared with the activities of already synthesized compounds and of drugs in use. Lots of the newly synthesized compounds showed promising antiprotozoal properties and selectivity, some of them exhibited even higher antiplasmodial activity than chloroquine. Structure-activity relationships were discussed.
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• 出版日期2016-2