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To evade the possible toxicity associated with the formation of quinone-imine metabolite in amodiaquine (AQ), the para -hydroxyl group was replaced with a -F atom, and the resulting 4'-fluoro-amodiaquine (FAQ) was hybridized with substituted pyrimidines. The synthesized FAQ-pyrimidines displayed better in vitro potency than chloroquine (CQ) against the resistant P. falciparum strain (Dd2), exhibiting up to 47.3-fold better activity (IC 50 : 4.69 nM) than CQ (IC 50 : 222 nM) and 2.8-fold better potency than artesunate (IC 50 : 13.0 nM). Twelve compounds exhibited better antiplasmodial activity than CQ against the CQ-sensitive (NF54) strain. Two compounds were evaluated in vivo against a P. berghei -mouse malaria model. Mechanistic heme-binding studies, computational docking studies against Pf -DHFR and in vitro microsomal stability studies were performed for the representative molecules of the series to assess their antimalarial efficacy.

Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ–Pyrimidines