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Malaria is one of the three major serious infectious diseases in the world. As the area affected by malaria includes a large proportion of developing countries, there is a need for new antimalarials that can be synthesized and supplied inexpensively. To generate low-cost antimalarials, the MAP series 6-10, bis-cation dimers, synthesized by amidating the carboxyl group of isonicotinic acid (11) with various amines and by cationizing the nitrogen atoms of the pyridine ring with the corresponding alkyl bromides, were designed. This design enabled expansion of the structural variations of bis-cation-type antimalarial compounds. The compounds bearing alkyl or phenyl groups in the amide moieties showed remarkable antimalarial activities in vitro. Moreover, 1,1'-(1,12-dodecanediyl)bis[4-[(buthylamino)carbonyl]pyridinium bromide], MAP-412 (6 d), exhibited a potent antimalarial activity (ED(50)=8.2 mg kg(-1)). Being prepared at low cost, our bis-cation-type antimalarial compounds may be useful as lead compounds for inexpensive antimalarials.

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The cover picture shows a human affected with malaria, the disease vector Anopheles, a map from the WHO showing areas of malaria risk, and MAP‐412, an antimalarial compound developed in our group. As the map shows, regions affected by malaria include a large proportion of developing countries. Therefore, there is a need for new antimalarials that can be synthesized and supplied inexpensively. Prepared in just two steps from an inexpensive starting material, isonicotinic acid, our bis‐cationic antimalarial compounds may be useful as leads for inexpensive antimalarials. For details, see the Full Paper by H. Kakuta et al. on p. 1527 ff. (Cover design by H.K.)