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 (S_NAr)-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