Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates. Issue 11 (18th October 2018)

• Record Type: Journal Article
• Authors: d'Orchymont, Faustine; Hess, Jeannine; Panic, Gordana; Jakubaszek, Marta; Gemperle, Lea; Keiser, Jennifer; Gasser, Gilles
• Is Part Of: MedChemComm. Volume 9:Issue 11(2018)
• Page Start: 1905
• Page End: 1909
• Publication Date: 2018-10-18
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c8md00396c
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described. Abstract : 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 and4 ) 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 of3 and4 to S. mansoni -infected mice did not significantly reduce worm burden, contrary to mefloquine.