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KMID : 0043320150380081455
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Archives of Pharmacal Research
2015 Volume.38 No. 8 p.1455 ~ p.1467
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Synthesis and antiprotozoal activities of new 3-azabicyclo[3.2.2]nonanes
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Ahmad Sarfraz
Seebache Werner
Wolkinger Volker
Presser Armin
Faist Johanna
Kaiser Marcel
Brun Reto
Saf Robert
Weis Robert
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Abstract
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Some antimalarial agents in use typically bear basic side chains as ligands. Such ligands were attached to the amino substituent of a bridgehead atom of already antiprotozoal active 3-azabicyclo[3.2.2]nonanes. Structure verification was done by NMR measurements. The new compounds were tested for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparumK1 (multiresistant) and Trypanosoma brucei rhodesiense as well as for their cytotoxicity against L6 cells. Their activities are compared to those of already prepared compounds and 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, Antiprotozoal activity, Physicochemical properties, Structure?activity relationships
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