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Some novel derivatives of 3-(3-(7-chloroquinolin-4-ylamino)propyl)-1,3-thiazinan-4-one were synthesized and characterized by their physical and spectral data. All the synthesized compounds were subsequently screened for in vitro antimalarial activity against chloroquine sensitive strain of Plasmodium falciparum (RKL-2) employing chloroquine as the reference drug. Most of the synthesized compounds exhibited mild to moderate susceptibilities towards the parasite in comparison to the standard. It was found that antimalarial activity of 3-(3-(7-chloroquinolin-4-ylamino)propyl)-2-(4-bromophenyl)-1,3-thiazinan-4-one was marginally superior than all the compounds evaluated.