Efficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities.

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A novel three-component, two-step, one-pot nucleophilic aromatic substitution (SNAr)-intramolecular cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin analogs was synthesized. The antimalarial activities of these compounds were evaluated against asexual parasites using a growth inhibition assay and gametocytes using a viability assay.


Li, Hao; Sun, Wei; Huang, Xiuli; Lu, Xiao; Patel, Paresma R; Kim, Myunghoon; Orr, Meghan J; Fisher, Richard M; Tanaka, Takeshi Q; McKew, John C; Simeonov, Anton; Sanderson, Philip; Zheng, Wei; Williamson, Kim C; Huang, Wenwei;

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