Derquantel is an anthelmintic spiroindole that acts as a nicotinic acetylcholine receptor antagonist, causing flaccid paralysis and expulsion of nematodes. A combination of derquantel and the macrocyclic lactone, abamectin , has been found to have synergistic anthelmintic effects against gastrointestinal nematode parasites in sheep.
Derquantel is a semi-synthetic paraherquamide analogue prepared by removal of the 2-oxo group in a four-step sequence of N-protection, reduction, N-deprotection and a final reduction. Derquantel isa potent nematocide and was the first paraherquamide to be successfully commercialised in combination with avermectin. Derquantel, like other paraherquamides, induces a flaccid paralysis in nematodes thought to be due to inhibition of nicotinic acetylcholine receptors acting as an antagonist of acetylcholine.
ChEBI: Derquantel is an azaspiro compound.
[1] M. ABONGWA. Curiouser and Curiouser: The Macrocyclic Lactone, Abamectin, Is also a Potent Inhibitor of Pyrantel/Tribendimidine Nicotinic Acetylcholine Receptors of Gastro-Intestinal Worms[J]. PLoS ONE, 2016, 11 1. DOI:
10.1371/journal.pone.0146854
