Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 2120975
Author(s) Faist, Johanna; Seebacher, Werner; Kaiser, Marcel; Brun, Reto; Saf, Robert; Weis, Robert
Author(s) at UniBasel Brun, Reto
Kaiser, Marcel
Year 2013
Title Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom
Journal Bioorganic & medicinal chemistry : a Tetrahedron publication for the rapid dissemenination of full original research papers and critical reviews on biomolecular chemistry, medicinal chemistry and related disciplines
Volume 21
Number 17
Pages / Article-Number 4988-96
Keywords 4-(4-Methylpiperazin-1-yl)bicyclo[2.2.2]octanes, 5-(4-Methylpiperazin-1-yl)-2-azabicyclo[3.2.2]nonanes, Plasmodium falciparum, Trypanosoma brucei rhodesiense
Abstract ω-Aminoacyl and -alkyl derivatives of 4-(4-methylpiperazin-1-yl)bicyclo[2.2.2]octan-2-amines and of 5-(4-methylpiperazin-1-yl)-2-azabicyclo[3.2.2]nonanes were prepared and their activities were examined in vitro against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). Some of the newly synthesized compounds showed very promising antiprotozoal activity and selectivity. A few of the alkylamino-2-azabicyclo[3.2.2]nonanes exhibited high antiplasmodial activity, whereas a single bicyclo[2.2.2]octane derivative was the most potent antitrypanosomal compound. The results of the newly synthesized compounds were compared with the activities of already synthesized compounds and of drugs in use. Structure-activity relationships were discussed.
Publisher Elsevier
ISSN/ISBN 0968-0896
edoc-URL http://edoc.unibas.ch/dok/A6165317
Full Text on edoc No
Digital Object Identifier DOI 10.1016/j.bmc.2013.06.059
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/23880082
ISI-Number WOS:000323294600013
Document type (ISI) Journal Article
 
   

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