Assessing the anthelmintic activity of pyrazole-5-carboxamide derivatives against Haemonchus contortus.

ABSTRACT:

Background

In this study, we tested five series of pyrazole-5-carboxamide compounds (n = 55) for activity against parasitic stages of the nematode Haemonchus contortus (barber's pole worm), one of the most pathogenic parasites of ruminants.

Methods

In an optimised, whole-organism screening assay, using exsheathed third-stage (xL3) and fourth-stage (L4) larvae, we measured the inhibition of larval motility and development of H. contortus.

Results

Amongst the 55 compounds, we identified two compounds (designated a-15 and a-17) that reproducibly inhibit xL3 motility as well as L4 motility and development, with IC₅₀ values ranging between ~3.4 and 55.6 μM. We studied the effect of these two 'hit' compounds on mitochondrial function by measuring oxygen consumpti

SUBMITTER: Jiao Y 

PROVIDER: S-EPMC5452367 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature