Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates.
- d'Orchymont F Department of Chemistry , University of Zurich , Winterthurerstrasse 190 , CH-8057 Zurich , Switzerland.
- Hess J Department of Chemistry , University of Zurich , Winterthurerstrasse 190 , CH-8057 Zurich , Switzerland.
- Panic G Department of Medical Parasitology and Infection Biology , Swiss Tropical and Public Health Institute , CH-4051 , Basel , Switzerland . Email: jennifer.keiser@unibas.ch.
- Jakubaszek M Laboratory for Inorganic Chemical Biology , Chimie ParisTech , PSL University , F-75005 Paris , France . Email: gilles.gasser@chimieparistech.psl.eu.
- Gemperle L Department of Chemistry , University of Zurich , Winterthurerstrasse 190 , CH-8057 Zurich , Switzerland.
- Keiser J Department of Medical Parasitology and Infection Biology , Swiss Tropical and Public Health Institute , CH-4051 , Basel , Switzerland . Email: jennifer.keiser@unibas.ch.
- Gasser G Laboratory for Inorganic Chemical Biology , Chimie ParisTech , PSL University , F-75005 Paris , France . Email: gilles.gasser@chimieparistech.psl.eu.
- 2018-12-21
Published in:
- MedChemComm. - 2018
English
We present the design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the organic antimalarial mefloquine, a drug also known for its antischistosomal activity. The two metallocenyl derivatives prepared (3 and 4) demonstrated comparable activity to mefloquine against adult-stage Schistosoma mansoni in vitro. Importantly, both compounds were found to have lower toxicity in all cell lines than mefloquine itself. Administration of a 200 mg kg-1 oral dose of 3 and 4 to S. mansoni-infected mice did not significantly reduce worm burden, contrary to mefloquine.
- Language
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- English
- Open access status
- green
- Identifiers
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- DOI 10.1039/c8md00396c
- PMID 30568758
- Persistent URL
- https://sonar.ch/global/documents/127260
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