Screening and hit evaluation of a chemical library against blood-stage Plasmodium falciparum.

ABSTRACT:

Background

In view of the need to continuously feed the pipeline with new anti-malarial agents adapted to differentiated and more stringent target product profiles (e.g., new modes of action, transmission-blocking activity or long-duration chemo-protection), a chemical library consisting of more than 250,000 compounds has been evaluated in a blood-stage Plasmodium falciparum growth inhibition assay and further assessed for chemical diversity and novelty.

Methods

The selection cascade used for the triaging of hits from the chemical library started with a robust three-step in vitro assay followed by an in silico analysis of the resulting confirmed hits. Upon reaching the predefined requirements for selectivity and potency, the set of hits was subjected to computational analysi

SUBMITTER: Avery VM 

PROVIDER: S-EPMC4094919 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature