3-Halo Chloroquine Derivatives Overcome Plasmodium falciparum Chloroquine Resistance Transporter-Mediated Drug Resistance in P. falciparum |
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| Authors: | Sonia Edaye Dagobert Tazoo D Scott Bohle Elias Georges |
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| Institution: | aInstitute of Parasitology, McGill University, Ste. Anne de Bellevue, Quebec, Canada;bDepartment of Chemistry, McGill University, Montreal, Quebec, Canada |
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| Abstract: | Polymorphism in the Plasmodium falciparum chloroquine resistance transporter (PfCRT) was shown to cause chloroquine resistance. In this report, we examined the antimalarial potential of novel 3-halo chloroquine derivatives (3-chloro, 3-bromo, and 3-iodo) against chloroquine-susceptible and -resistant P. falciparum. All three derivatives inhibited the proliferation of P. falciparum; with 3-iodo chloroquine being most effective. Moreover, 3-iodo chloroquine was highly effective at potentiating and reversing chloroquine toxicity of drug-susceptible and -resistant P. falciparum. |
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