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The antiprotozoal potencies of newly prepared 3-azabicyclo[3.2.2]nonanes
Sarfraz Ahmad,Werner Seebacher,Johanna Faist,Marcel Kaiser,Reto Brun,Robert Saf,Robert Weis 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.10
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
Synthesis and antiprotozoal activities of new 3-azabicyclo[3.2.2]nonanes
Sarfraz Ahmad,Werner Seebacher,Volker Wolkinger,Armin Presser,Johanna Faist,Marcel Kaiser,Reto Brun,Robert Saf,Robert Weis 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.8
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 falciparum K1 (multiresistant) and Trypanosoma brucei rhodesiense as well as for their cytotoxicity against L6 cells. Theiractivities are compared to those of already prepared compounds and structure–activity relationships are discussed.
Robert Weis,Heinrich Berger,Marcel Kaiser,Reto Brun,Robert Saf,Werner Seebacher 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.6
New alkenes, aziridines, and diamines were prepared from antiprotozoal 4-dialkylaminobicyclo[ 2.2.2]octan-2-imines to investigate the influence of several functional groups in position 2 of the ring skeleton on the antitrypanosomal and antiplasmodial activities. They were synthesized from 4-dialkylaminobicyclo[2.2.2]octan-2-imines and tested for their activities against Trypanosoma b. rhodesiense and Plasmodium falciparum K1 (resistant to chloroquine and pyrimethamine) using in vitro microplate assays. 4-Aminobicyclo[2.2.2]oct-2-enes and 3-azatricyclo[ 3.2.2.02,4]nonylamines exhibit similar antiprotozoal activities as 4-aminobicyclo[2.2.2] octanes. 4-Aminobicyclo[2.2.2]oct-2-ylamines and their N-benzyl derivatives showed decreased antiplasmodial but enhanced antitrypanosomal (IC50 = 0.22-0.41 μM) activities compared to their parent oximes and to formerly synthesized 4-amino-2-azabicyclo[3.2.2]nonanes. Some of the 4-aminobicyclo[2.2.2]oct-2-ylamines exhibit moderate in vivo activity in mice against Trypanosoma brucei brucei.
Weis, Robert,Berger, Heinrich,Kaiser, Marcel,Brun, Reto,Saf, Robert,Seebacher, Werner 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.6
New alkenes, aziridines, and diamines were prepared from antiprotozoal 4-dialkylaminobicyclo[2.2.2]octan-2-imines to investigate the influence of several functional groups in position 2 of the ring skeleton on the antitrypanosomal and antiplasmodial activities. They were synthesized from 4-dialkylaminobicyclo[2.2.2]octan-2-imines and tested for their activities against Trypanosoma b. rhodesiense and Plasmodium falciparum $K_1$ (resistant to chloroquine and pyrimethamine) using in vitro microplate assays. 4-Aminobicyclo[2.2.2]oct-2-enes and 3-azatricyclo[$3.2.2.0^{2,4}$]nonylamines exhibit similar antiprotozoal activities as 4-aminobicyclo[2.2.2] octanes. 4-Aminobicyclo[2.2.2]oct-2-ylamines and their N-benzyl derivatives showed decreased antiplasmodial but enhanced antitrypanosomal ($IC_{50}\;=\;0.22-0.41\;{\mu}M$) activities compared to their parent oximes and to formerly synthesized 4-amino-2-azabicyclo[3.2.2]nonanes. Some of the 4-aminobicyclo[2.2.2]oct-2-ylamines exhibit moderate in vivo activity in mice against Trypanosoma brucei brucei.