Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidatesElectronic supplementary information (ESI) available. See DOI: 10.1039/c8md00396c
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 activ...
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| creator | d'Orchymont, Faustine Hess, Jeannine Panic, Gordana Jakubaszek, Marta Gemperle, Lea Keiser, Jennifer Gasser, Gilles |
| description | 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.
The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described. |
| doi_str_mv | 10.1039/c8md00396c |
| format | Article |
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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.
The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.</description><identifier>ISSN: 2040-2503</identifier><identifier>EISSN: 2040-2511</identifier><identifier>DOI: 10.1039/c8md00396c</identifier><language>eng</language><creationdate>2018-11</creationdate><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,778,782,27907,27908</link.rule.ids></links><search><creatorcontrib>d'Orchymont, Faustine</creatorcontrib><creatorcontrib>Hess, Jeannine</creatorcontrib><creatorcontrib>Panic, Gordana</creatorcontrib><creatorcontrib>Jakubaszek, Marta</creatorcontrib><creatorcontrib>Gemperle, Lea</creatorcontrib><creatorcontrib>Keiser, Jennifer</creatorcontrib><creatorcontrib>Gasser, Gilles</creatorcontrib><title>Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidatesElectronic supplementary information (ESI) available. See DOI: 10.1039/c8md00396c</title><description>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.
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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.
The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.</abstract><doi>10.1039/c8md00396c</doi><tpages>5</tpages></addata></record> |
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| source | Royal Society Of Chemistry Journals 2008-; PubMed Central |
| title | Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidatesElectronic supplementary information (ESI) available. See DOI: 10.1039/c8md00396c |
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