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

ABSTRACT: 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.

SUBMITTER: Li H

PROVIDER: S-EPMC5870878 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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

Li Hao H Sun Wei W Huang Xiuli X Lu Xiao X Patel Paresma R PR Kim Myunghoon M Orr Meghan J MJ Fisher Richard M RM Tanaka Takeshi Q TQ McKew John C JC Simeonov Anton A Sanderson Philip E PE Zheng Wei W Williamson Kim C KC Huang Wenwei W

ACS combinatorial science 20171027 12

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. ...[more]

PMID: 29024590

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