Journal article

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

Yaqing Jiao, Sarah Preston, Hongjian Song, Abdul Jabbar, Yuxiu Liu, Jonathan Baell, Andreas Hofmann, Dana Hutchinson, Tao Wang, Anson V Koehler, Gillian M Fisher, Katherine T Andrews, Benoit Laleu, Michael J Palmer, Jeremy N Burrows, Timothy NC Wells, Qingmin Wang, Robin B Gasser



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 '..

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Awarded by Victoria Life Sciences Computation Initiative, Australia (VLSCI)

Funding Acknowledgements

The present study was funded by the Australian Research Council (ARC), the Wellcome Trust (RBG) and National Health and Medical Research Council of Australia (NHMRC), and supported by a Victoria Life Sciences Computation Initiative, Australia (VLSCI; grant no. VR0007) on its Peak Computing Facility at The University of Melbourne, Australia, an initiative of the Victorian Government, Australia. GMF was supported by a Postdoctoral Fellowship and New Researcher Grant from Griffith University.