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Table 6 Priorities – exploiting high throughput screening hits quickly

From: CRIMALDDI: a prioritized research agenda to expedite the discovery of new anti-malarial drugs

Removing key roadblocks to future progress • Establish a single repository for compounds identified as positive screening hits and increase availability of these compound “powders” including increased medicinal chemistry resources to synthesize the compounds
Speeding-up drug discovery • Continue routine screening of compound libraries and prioritization of positive hits in secondary screening. Agrochemical libraries are a particular priority
• Emphasize development of better understanding of absorption, distribution, metabolism, and elimination (ADME) and toxicology of positive hits early in the discovery process
• Use information on parasite resistance to chemical classes to probe underlying biological processes
  • Evaluate the speed of action and stage specificity of current HTS hits (currently 15.000‒20,000 novel chemotypes) to identify new chemotypes with similar pharmacodynamics to artemisinins. This should include evaluation against parasites with stable resistance to artemisinins (and other anti-malarials) and parasites arising from resistance “hot spots”