1028344-61-7Relevant articles and documents
Organometallic Derivatization of the Nematocidal Drug Monepantel Leads to Promising Antiparasitic Drug Candidates
Hess, Jeannine,Patra, Malay,Rangasamy, Loganathan,Konatschnig, Sandro,Blacque, Olivier,Jabbar, Abdul,Mac, Patrick,Jorgensen, Erik M.,Gasser, Robin B.,Gasser, Gilles
supporting information, p. 16602 - 16612 (2016/11/09)
The discovery of novel drugs against animal parasites is in high demand due to drug-resistance problems encountered around the world. Herein, the synthesis and characterization of 27 organic and organometallic derivatives of the recently launched nematocidal drug monepantel (Zolvix) are described. The compounds were isolated as racemates and were characterized by1H,13C, and19F NMR spectroscopy, mass spectrometry, and IR spectroscopy, and their purity was verified by microanalysis. The molecular structures of nine compounds were confirmed by X-ray crystallography. The anthelmintic activity of the newly designed analogues was evaluated in vitro against the economically important parasites Haemonchus contortus and Trichostrongylus colubriformis. Moderate nematocidal activity was observed for nine of the 27 compounds. Three compounds were confirmed as potentiators of a known monepantel target, the ACR-23 ion channel. Production of reactive oxygen species may confer secondary activity to the organometallic analogues. Two compounds, namely, an organic precursor (3 a) and a cymantrene analogue (9 a), showed activities against microfilariae of Dirofilaria immitis in the low microgram per milliliter range.
THE USE OF AMINOACETONITRIL COMPOUNDS IN THE CONTROL OF ENDOPARASITES IN WARM- BLOOD ANIMALS.
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Page/Page column 31, (2008/12/05)
The invention relates to the use of aminoacetonitrile compounds of formula (I) wherein A, R4, R5, m, Y1, Y2, Y3, Y4 and Y5 have the significances given in claim 1, in the control of endoparasites, especially helminths, in warm-blooded productive livestock and domestic animals.
AMIDOACETONITRILE DERIVATIVES
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Page/Page column 31, (2008/06/13)
The invention relates to compounds of the general formula (I) wherein X, Y and W have the significances given in claim 1 and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable f