Search for new pharmacophores for antimalarial activity. Part III: Synthesis and bioevaluation of new 6-thioureido-4-anilinoquinazolines

Syntheses and in vitro antimalarial evaluation of 42 new thioureidoquinazolines have been carried out. Several analogs showed promising antimalarial effect in the in vitro investigation against chloroquine-sensitive 3D7 strain of Plasmodium falciparum whereas one of the compounds shows 50% curative effect in the mouse model at an oral dose of 100 mg/kg × 4 days against multidrug resistant Plasmodium yoelii nigeriensis.

Graphical abstractSyntheses and in vitro antimalarial evaluation of 42 new thioureidoquinazolines against CQS P. falciparum is described. One of the compounds shows 50% curative effect against MDR P. yoelii nigeriensis.Figure optionsDownload full-size imageDownload as PowerPoint slide