Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities

Bioorganic & Medicinal Chemistry Letters
Werner SeebacherRobert Weis

Abstract

Several bicyclic compounds, 3-azabicyclo[3.2.2]nonanes, have been prepared. The new compounds were tested for their activities against one strain of the causative organism of Malaria tropica, Plasmodium falciparum K1, which is resistant against chloroquine and pyrimethamine. In addition, their cytotoxicity and their activity against the pathogen of the East African form of sleeping sickness, Trypanosoma brucei rhodesiense, were investigated. Structure-activity relationships are discussed considering data of readily prepared compounds. For the first time, a distinct in vivo activity was observed against Plasmodium berghei in a mouse model. The active compound was further investigated.

References

Oct 17, 2009·Lancet·Reto BrunChristian Burri
Apr 27, 2010·Lancet·Jane CrawleyFrançois Nosten

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Citations

Sep 3, 2016·Archives of Pharmacal Research·Sarfraz AhmadRobert Weis
Oct 31, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Seong-Min LeeDongyun Shin
Sep 17, 2019·European Journal of Medicinal Chemistry·Anudeep K NarulaLalit M Nainwal
Aug 8, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Anshula SharmaBaljinder Kaur

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