Malaria remains a formidable global problem. Although substantial progress has been made in efforts to combat and to eliminate this protozoan scourge, much remains to be done. This review dealing with the chemotherapy of malaria presents: a brief resume of historical aspects relating to the development of synthetic antimalarial drugs; a discussion of apposite considerations with respect to parasites that cause human malaria, classification of antimalarial drugs, and terminology; a summary of available information concerning the uses and effects of quinine and widely employed synthetic antimalarial drugs; a short account of certain other antimalarial agents, some developed recently, that are of considerable experimental interest; and a discussion of resistance of malaria parasites to drugs, with particular emphasis on recently detected parasites that are resistant to chloroquine and to other synthetic antimalarial drugs.