New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds

Faist, J. and Seebacher, W. and Saf, R. and Brun, R. and Kaiser, M. and Weis, R.. (2012) New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds. European journal of medicinal chemistry, 47 (1). pp. 510-519.

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Official URL: http://edoc.unibas.ch/dok/A6094297

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The 4-methylpiperazinyl group was inserted as substituent at the bridgehead of bicyclic compounds or as terminal group of their aminoacyl and aminoalkyl side chains. The new compounds were tested in vitro for their activities against the multidrug-resistant K(1) strain of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). The results were compared to those of formerly prepared analogues and of drugs in use. A couple of bicyclo-octyl omega-(4-piperazin-1-yl)alkanoates showed high antitrypanosomal (IC(50)>/=0.087muM) and antiplasmodial activity (IC(50)>/=0.06muM). The most active omega-(4-methylpiperazin-1-yl)alkyl-2-azabicyclo-nonane possessed higher antiplasmodial activity (IC(50)>/=0.023muM) and selectivity (S.I.=IC(50) (Cytotox.)/IC(50) (P. falciparum)=2188) than the antimalarial drug chloroquine (IC(50)=0.15muM, S.I.=1257)
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology (MPI) > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Kaiser, Marcel
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:05 Dec 2017 10:08
Deposited On:19 Jul 2013 07:39

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