Journal article

Assessment of the nematocidal activity of metallocenyl analogues of monepantel

Jeannine Hess, Malay Patra, Abdul Jabbar, Vanessa Pierroz, Sandro Konatschnig, Bernhard Spingler, Stefano Ferrari, Robin B Gasser, Gilles Gasser

DALTON TRANSACTIONS | ROYAL SOC CHEMISTRY | Published : 2016

Abstract

In this study, we present the design, synthesis, characterization and biological evaluation of structurally new ferrocenyl and ruthenocenyl derivatives of the organic anthelmintic monepantel (Zolvix®). All seven metallocenyl derivatives prepared (4a/b, 5a/b, 6a/b and 7) were isolated as racemates and characterized by 1H, 13C and 19F NMR spectroscopies, mass spectrometry, IR spectroscopy and elemental microanalysis. The molecular structures of four compounds (4a/b, 6a and 7) were further confirmed by X-ray crystallography. The biological activities of the organometallic intermediates (4a/b) and organometallic derivatives of monepantel (5a/b, 6a/b and 7) were evaluated in vitro using parasitic..

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Grants

Awarded by Swiss National Science Foundation


Funding Acknowledgements

This work was financially supported by the Swiss National Science Foundation (Professorships No. PP00P2_133568 and PP00P2_157545 to G. G.), the University of Zurich (G. G., S. F.), the Stiftung fur wissenschaftliche Forschung of the University of Zurich (G. G., S. F.), the Novartis Jubilee Foundation (G. G.), the Kurt u. Senta Hermann Stiftung (S. F.) and the Swiss Government Excellence Scholarship for Postdoctoral Researcher (R. L.). R. B. G.'s research program is supported by the Australian Research Council (ARC), the National Health and Medical Research Council (NHMRC), Melbourne Water Corporation, Yourgene Bioscience and the Alexander von Humboldt Foundation and The University of Melbourne. R. B. G. is a grateful recipient of Professorial Humboldt Research Awards. The authors would like to thank Dr Jacques Bouvier (Novartis Animal Health, St-Aubin, Switzerland) and Dr Noelle Gauvry (Novartis Animal Health, Basel, Switzerland) for their help with the biological assays.