Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes

Heinrich Berger; Werner Seebacher; Robert Saf; Marcel Kaiser; Reto Brun; Robert Weis

doi:10.1016/j.bmcl.2006.07.057

Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5457-61. doi: 10.1016/j.bmcl.2006.07.057. Epub 2006 Aug 2.

Authors

Heinrich Berger¹, Werner Seebacher, Robert Saf, Marcel Kaiser, Reto Brun, Robert Weis

Affiliation

¹ Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitätsplatz 1, A-8010 Graz, Austria.

PMID: 16889962
DOI: 10.1016/j.bmcl.2006.07.057

Abstract

The in vitro activity of newly synthesized bis-(chlorophenyl)-azabicyclo[3.2.2]nonanes and bis-(chlorophenyl)-bicyclo[2.2.2]octanes against Plasmodium falciparum K(1) (resistant to chloroquine and pyrimethamine) and Trypanosoma brucei rhodesiense was investigated. Especially the bis-(chlorophenyl)-azabicyclo[3.2.2]nonanes exhibit promising antitrypanosomal activity and were tested in vivo against Trypanosoma brucei brucei featuring moderate activities.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antiprotozoal Agents / chemical synthesis
Antiprotozoal Agents / chemistry
Antiprotozoal Agents / pharmacology*
Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
Bridged Bicyclo Compounds, Heterocyclic / chemistry
Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
In Vitro Techniques
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium falciparum / drug effects*
Stereoisomerism
Structure-Activity Relationship
Trypanosoma brucei brucei / drug effects*
Trypanosoma brucei rhodesiense / drug effects*

Substances

Antiprotozoal Agents
Bridged Bicyclo Compounds, Heterocyclic