pntd.0008630.g001.tif (265.98 kB)

The screening pipeline utilised in this anti-infective study.

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posted on 19.10.2020, 17:33 by Helen Whiteland, Alessandra Crusco, Lisa W. Bloemberg, Jamie Tibble-Howlings, Josephine Forde-Thomas, Avril Coghlan, Patrick J. Murphy, Karl F. Hoffmann

A total of 14 compounds were initially screened against S. mansoni schistosomula at a final concentration of 10 μM. Hits were subsequently subjected to dose response titrations with the most effective anti-schistosomula compound (Compound 1) subsequently being used as a template for the preparation of further derivatives (compounds 2–9). Compounds 2–9 were subsequently subjected to dose response titrations against schistosomula and adult worms. The most effective compounds (original compound 1 and analogue 3) were next titrated against juvenile worms. Finally, compounds 1, 3, 5 and 6 were additionally titrated against both Gram+ (S. aureus) and Gram- (E. coli) bacterial exemplars.