figshare
Browse

The screening pipeline utilised in this anti-infective study.

Download (265.98 kB)
figure
posted on 2020-10-19, 17:33 authored by Helen Whiteland, Alessandra Crusco, Lisa W. Bloemberg, Jamie Tibble-Howlings, Josephine Forde-Thomas, Avril Coghlan, Patrick J. Murphy, Karl F. Hoffmann
<p>A total of 14 compounds were initially screened against <i>S</i>. <i>mansoni</i> schistosomula at a final concentration of 10 μM. Hits were subsequently subjected to dose response titrations with the most effective anti-schistosomula compound (Compound <b>1</b>) subsequently being used as a template for the preparation of further derivatives (compounds <b>2–9</b>). Compounds <b>2–9</b> were subsequently subjected to dose response titrations against schistosomula and adult worms. The most effective compounds (original compound <b>1</b> and analogue <b>3</b>) were next titrated against juvenile worms. Finally, compounds <b>1</b>, <b>3</b>, <b>5</b> and <b>6</b> were additionally titrated against both Gram<sup>+</sup> (<i>S</i>. <i>aureus</i>) and Gram<sup>-</sup> (<i>E</i>. <i>coli</i>) bacterial exemplars.</p>

History