We report the synthesis, in vitro antiprotozoal (against Plasmodium and Leishmania), antimicrobial, cytotoxicity (Vero and MetHb-producing properties), and in vivo antimalarial activities of two series of 8-quinolinamines. N1-{4-[2-(tert-Butyl)-6-methoxy-8-quinolylamino] pentyl}-(2S/2R)-2-aminosubstitutedamides (21–33) and N1-[4-(4-ethyl-6-methoxy-5- pentyloxy-8-quinolylamino) pentyl]-(2S/2R)-2-aminosubstitutedamides (51–63) were ...