Synthesis and in vitro antiplasmodial evaluation of some isoquine analogues

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Isoquine is the regioisomer of amodiaquine that can not form hepato and haematotoxic active metabolites by biotransformation unlike amodiaquine. In present investigation, five new isoquine analogues were synthesized by a two-step method, characterized by spectral analyses and subsequently evaluated in vitro against the chloroquine sensitive RKL-2 strain of Plasmodium falciparum by JSB staining method. All synthesized compounds demonstrated differential extent of antiplasmodial activity against the test parasites. However, no compound was found to exhibit better antiplasmodial profile as compared to chloroquine.

Isoquine; antiplasmodial; RKL-2; Plasmodium falciparum; JSB staining