The antiprotozoal potencies of newly prepared 3-azabicyclo[3.2.2]nonanes
3-Azabicyclo[3.2.2]nonanes are already reported as antiprotozoal agents. Structural variations were performed by attachment of several basic side chains, being part of drugs in use, to the ring nitrogen. The structures of the new compounds were established using one and two dimensional NMR measurements. All compounds were investigated for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum K 1 (multiresistant) and Trypanosoma brucei rhodesiense. Their cytotoxicity was assessed against L6 cells. The results are compared to the activities of formerly synthesized compounds. Structure–activity relationships are discussed.
Keywords3-Azabicyclo[3.2.2]nonanes Basic side chains Antimalarial activity Antitrypanosomal activity Structure–activity relationships
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