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KMID : 0043320160390101391
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Archives of Pharmacal Research
2016 Volume.39 No. 10 p.1391 ~ p.1403
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The antiprotozoal potencies of newly prepared 3-azabicyclo[3.2.2]nonanes
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Ahmad Sarfraz
Seebacher Werner
Faist Johanna
Kaiser Marcel
Brun Reto
Saf Robert
Weis Robert
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Abstract
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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 K1 (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.
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KEYWORD
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3-Azabicyclo[3.2.2]nonanes, Basic side chains, Antimalarial activity, Antitrypanosomal activity, Structure?activity relationships
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