Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds

► 29 imidazoisoindoles, imidazobenzimidazoles and isoindolinones synthesized. ► IC50 values against 3D7 Plasmodium falciparum ranged between 60 nM and >35 mM. ► 7 imidazoisoindoles assayed on mice infected with Plasmodium berghei. ► Up to 87% parasitemia inhibition on the 5th day, after 4 daily i.p. 25 mg/kg/day.