When molecular targets are lacking, a phenotypic-based drug discovery approach may prove useful. This is how PZQ’s anthelmintic activity was discovered by inducing characteristic effects to the worms in vitro that could be translated into in vivo efficacy. In this chapter we portray how compounds are tested against Schistosoma mansoni in vitro and in vivo. As an example for successful phenotyping screening, we describe the structure–activity relationship of praziquantel.

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In Vitro and In Vivo Activity of Praziquantel Against Schistosome Worms

  • Thomas Spangenberg,
  • Jennifer Keiser

摘要

When molecular targets are lacking, a phenotypic-based drug discovery approach may prove useful. This is how PZQ’s anthelmintic activity was discovered by inducing characteristic effects to the worms in vitro that could be translated into in vivo efficacy. In this chapter we portray how compounds are tested against Schistosoma mansoni in vitro and in vivo. As an example for successful phenotyping screening, we describe the structure–activity relationship of praziquantel.