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Seven <jats:italic>N<\/jats:italic>\u2010substituted azaozonides exhibited high antimalarial activity against the chloroquine\u2010sensitive 3D7 strain of <jats:italic>P. falciparum<\/jats:italic>, with IC<jats:sub>50<\/jats:sub>\u2009&lt;\u20091\u2009\u03bcM. The lead compound <jats:bold>22<\/jats:bold> showed IC<jats:sub>50<\/jats:sub>\u2009=\u20090.07\u2009\u03bcM and selectivity index of 1428. Most aminoperoxides were generally non\u2010cytotoxic to both normal and cancer liver and lung cells. Only two azaozonides exhibited moderate cytotoxicity on HepG2 cell line (<jats:bold>2<\/jats:bold>: IC<jats:sub>50<\/jats:sub>\u2009=\u20094.12\u2009\u03bcM, <jats:bold>40<\/jats:bold>: 9.95\u2009\u03bcM), while one azaozonide <jats:bold>2<\/jats:bold> had an IC<jats:sub>50<\/jats:sub>\u2009=\u20095.56\u2009\u03bcM against A549 cell line. From this small library of 45 aminoperoxides, compound <jats:bold>22<\/jats:bold> was found to have antimalarial activity comparable to artemisinin and chloroquine used in medical practice. 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