() is a tick that causes huge economic losses in cattle. The indiscriminate use of acaricides has generated resistance to most compounds present on the market. Carvacrol and salicylic acid have been widely studied for their biological activities and have been evaluated in different strains of .
View Article and Find Full Text PDFBioorg Med Chem Lett
July 2014
A family of 15 N-substituted phenothiazines was designed, synthesized and their acaricidal activity against Rhipicephalus microplus was determined in vitro. The synthetic methodology is simple and can be employed in multigram scale. The rationale for the structure-based design of these compounds is the potential for azines and phenothiazine to engage in π-π interactions; these fragments, joined together by a short, flexible alkoxide linker, structurally resemble phenothiazine-based cholinesterase inhibitors, while their weak basicity implies a neutral active form, rather than a cationic one, thus facilitating penetration of the cuticle of ticks.
View Article and Find Full Text PDFRhipicephalus (Boophilus) microplus is a tick that causes huge economic losses in cattle. The indiscriminate use of acaricides has generated resistance to most compounds present on the market. This makes further investigation on other potential acaricides necessary, the in silico assay being an alternative to the design of new compounds.
View Article and Find Full Text PDFThe damage to the tegument of 3-week-old Fasciola hepatica was evaluated by scanning electron microscopy (SEM) following treatment with the 5-chloro-2-methylthio-6-(1-naphtyloxy)-1H-benzimidazole (called compound alpha) in its natural host. For the present study, flukes were raised in pelibuey sheep infected orally with metacercariae of F. hepatica; the parasites were recovered from the liver of the sacrificed sheep after 6, 12 and 24 h of treatment with compound alpha.
View Article and Find Full Text PDFOur objective was to determine by scanning electron microscopy the structural changes in the tegument of adult Fasciola hepatica after treatment with 5-chloro-2-methylthio-6-(1-naphtyloxy)-1 H-benzimidazole, called compound alpha, and its active metabolite sulphoxide, under in vitro and in vivo conditions. For the in vitro studies, flukes from sheep were exposed to 40 mg/l of compound alpha-sulphoxide over different incubation times. Flukes for the in vivo studies were raised in sheep treated orally with compound alpha and killed at different times post-treatment.
View Article and Find Full Text PDFThe aim of the present study was to determine the effective dose of an experimental fasciolicide called compound alpha or 5-chloro-2-methylthio-6-(1-napthyloxy)1H-benzimidazole in experimentally and naturally infected cattle. In the first experiment, 24 fluke-free heifers were each infected with 800 metacercariae of Fasciola hepatica and re-infected on day 45 with other 600 cysts per animal. On day 75, when the animals had 4- and 10-week-old flukes respectively, they were divided into four groups (G) of six animals each according to fluke egg counts.
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