title: Synthesis and endectocidal activity of novel 1-(arylsulfonyl)-1-[(trifluoromethyl)sulfonyl]methane derivatives.
abstract: We have recently synthesized a series of novel disulfonylmethane compounds that have shown anthelmintic and insecticidal (endectocidal) activity. Several analogues have shown activity against the internal nematode Haemonchus contortus. In sheep studies, these analogues have shown 100% control of this internal parasite at a 10 mg/kg rate. In vitro activity against the biting flies, Stomoxys calcitrans and Haematobia irritans, has been observed at rates as low as 25 and 2.3 ppm, respectively. Only marginal activity against the liver fluke Fasciola hepatica and Trichostrongylus colubriformis was seen. Respiratory control index values on rat liver mitochondria for this series suggested uncoupling of oxidative phosphorylation as a mechanism of action. Compound 1 is considered to be a promising agent for treatment of parasitized sheep.
authors.affiliation: Elanco Animal Health, Division of Eli Lilly and Company, Greenfield, Indiana 46140, USA.
authors.forename: D I
authors.initials: DI
authors.lastname: Wickiser
authors.forename: S A
authors.initials: SA
authors.lastname: Wilson
authors.forename: D E
authors.initials: DE
authors.lastname: Snyder
authors.forename: K R
authors.initials: KR
authors.lastname: Dahnke
authors.forename: C K
authors.initials: CK
authors.lastname: Smith
authors.forename: P J
authors.initials: PJ
authors.lastname: McDermott
mesh_terms: D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005210:Fasciola hepatica / Q000187:drug effects; D005849:Gerbillinae / Q000469:parasitology; D006188:Haemonchiasis / Q000188:drug therapy; D006189:Haemonchus / Q000187:drug effects; D009117:Muscidae / Q000187:drug effects; D012756:Sheep; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology; D014254:Trichostrongylus / Q000187:drug effects
chemical_list: D000871:Anthelmintics; D013450:Sulfones