Journal of Medicinal Chemistry p. 3295 - 3301 (1991)
Update date:2022-09-26
Topics:
Sjogren, Eric B.
Rider, Michael A.
Nelson, Peter H.
Bingham, Stanford
Poulton, Anthony L.
et al.
A series of α-cyano-β-hydroxypropenamides was prepared and tested for anthelmintic activity. α-Cyano-β-hydroxy-N-<4-(trifluoromethyl)phenyl>-3-<4-(trifluoromethyl)phenyl>propenamide (1) showed good activity against the nematode Nematospirodes dubius in a mixed parasite infection in mice; several of the analogues were also effective against the cestode Hymenolepis nana.In sheep trials, 1 caused 100percent reduction of the hematophagous nematode Haemonchus contortus after a single dose of 20 mg/kg but did not show satisfactory control of Trichostrongylus colubriformis or Ostertagia circumcincta.Against the liver fluke Fasciola hepatica, 1 suppressed egg production but only temporarily, suggesting that the adult flukes were not eliminated.Mechanism of action studies on 1 using Ascaris mitochondria showed it to be an uncoupler of oxidative phosphorylation.
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