THE PRESENT INVENTION RELATES TO NOVEL SUBSTITUTED 1, 2, 4-TRIOXANES USEFUL AS ANTI-MALARIAL AGENTS, AND HAVE GENERAL FORMULA 1, WHEREIN R₁ AND R₂ ARE SELECTED FROM THE GROUP CONSISTING OF A HYDROGEN, A C₁- ₁₁ ALKY GROUP R₃ AND R₄ ARE SELECTED FROM THE GROUP CONSISTING OF A HYDROGEN, A C₁- ₁₁ ALKY GROUP, A C₃-₁₀ ARYL GROUP, A C₁-₂ CO₂H CARBOXYALKYL GROUP AND X REPRESENTS HYDROGEN OR A LOWER ALKOXY GROUP HAVING 1 TO 6 CARBONS.