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Malaria is an infectious illness, affecting vulnerable populations in Third World countries. Inspired by natural products, indole alkaloids have been used as a nucleus to design new antimalarial drugs. So, eighteen oxindole derivatives,  aza  analogues were obtained with moderate to excellent yields. Also, the saturated derivatives of oxindole and  aza  derivatives  via  H 2 /Pd/C reduction were obtained in good yields, leading to racemic mixtures of each compound. Next, the inhibitory activity against  P. falciparum  of 18 compounds were tested, founding six compounds with IC 50  &lt; 20 µM. The most active of these compounds was  8c ; however, their unsaturated derivative  7c  was inactive. Then, a structure-activity relationship analysis was done, founding that focused LUMO lobe on the specific molecular zone is related to inhibitory activity against  P. falciparum . Finally, we found a potential inhibition of lactate dehydrogenase by oxindole derivatives, using molecular docking virtual screening.

3-aryl-indolinones derivatives as antiplasmodial agents: synthesis, biological activity and computational analysis