The newly obtained hybrids and associated intermediates were submitted to a first in vitro screening against a transgenic T. gondii strain constitutively expressing β-galactosidase (T. gondii β-gal) grown in human foreskin fibroblasts (HFF), while their cytotoxicity was evaluated in non-infected HFF by alamarBlue assay. Both tests were conducted at 0.1 and 1 µM. The compounds exhibiting interesting antiparasitic activity (90% tachyzoite proliferation inhibition) and low cytotoxicity (>50% HFF viability) at 1 µM were subjected to a T. gondii IC50 (half-maximal inhibitory concentration) determination, and HFF cytotoxicity assessment at 2.5 µM.