Antimalaria activity

Shaw states in a recent review that a number of anti-malarial drugs, which can also be used for the treatment of RA, actually exhibit pharmacological profiles akin to that of gold drugs, an observation indicating that common features exist between the mode of action of these anti-malarial and anti-arthritic drugs.37 Despite this, relatively little work has been devoted to exploring the possible application of gold complexes as anti-malarial agents. A series of metal complexes of the anti-malarial drugs Amodiaquine® (19) and Primaquine® (20) (Figure 26.7) were screened, in vitro, for activity against the parasitic protozoan Plasmodium falciparum, the causative agent for malaria.92 The complexation of these drugs to a metal centre, including Au(III), did not appear to influence greatly the minimum inhibitory values.92 More recently, a cationic phosphine-gold(I) chloroquine complex, [Ph3PAu(chloroquine)]PF6 (21) (Figure 26.7) was demonstrated to be active against the P. falciparum, in vitro, and P. berghei, both in vitro and in vivo.93 It is noteworthy that both of these strains are

OH NEt2 19

OH NEt2 19

PPha 21


Figure 26.7 Chemical structures of Amodiaquine® (19), Primaquine® (20), [Ph3PAu (chloroquine)]PF6 (21), Clotrimazole® (22) and Ketoconazole® (23)

resistant to Chloroquine®. In addition and importantly, it was shown that the presence of Au(I) gave rise to enhanced activity compared with other metal chloroquine complexes as well as Chloroquine Diphosphate®.93 Related Ph3PAu(I) complexes of Clotrimazole® (22) and Ketoconazole® (23), shown in Figure 26.7, have been evaluated for activity against Trypanosoma cruzi, the causative agent of Chagas disease, a major parasitic disease afflicting people in Latin America. As found in the study of the anti-malarial activity of the Au(I) complexes discussed earlier, the presence of the phosphinegold(I) moiety resulted in an enhancement of growth inhibitory activity.94

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