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- Title
A new class of anthelmintics effective against drug-resistant nematodes.
- Authors
Kaminsky, Ronald; Ducray, Pierre; Jung, Martin; Clover, Ralph; Rufener, Lucien; Bouvier, Jacques; Weber, Sandra Schorderet; Wenger, Andre; Wieland-Berghausen, Susanne; Goebel, Thomas; Gauvry, Noelle; Pautrat, François; Skripsky, Thomas; Froelich, Olivier; Komoin-Oka, Clarisse; Westlund, Bethany; Sluder, Ann; Mäser, Pascal
- Abstract
Anthelmintic resistance in human and animal pathogenic helminths has been spreading in prevalence and severity to a point where multidrug resistance against the three major classes of anthelmintics—the benzimidazoles, imidazothiazoles and macrocyclic lactones—has become a global phenomenon in gastrointestinal nematodes of farm animals. Hence, there is an urgent need for an anthelmintic with a new mode of action. Here we report the discovery of the amino-acetonitrile derivatives (AADs) as a new chemical class of synthetic anthelmintics and describe the development of drug candidates that are efficacious against various species of livestock-pathogenic nematodes. These drug candidates seem to have a novel mode of action involving a unique, nematode-specific clade of acetylcholine receptor subunits. The AADs are well tolerated and of low toxicity to mammals, and overcome existing resistances to the currently available anthelmintics.
- Subjects
ANTHELMINTICS; BENZIMIDAZOLES; HELMINTHS; MULTIDRUG resistance; DRUG development; NEMATODES; CHOLINERGIC receptors; NEUROTRANSMITTER receptors; MEDICAL research
- Publication
Nature, 2008, Vol 452, Issue 7184, p176
- ISSN
0028-0836
- Publication type
Article
- DOI
10.1038/nature06722