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ACS Comb Sci. 2017 Dec 11;19(12):748-754. doi: 10.1021/acscombsci.7b00119. Epub 2017 Oct 27.

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

Author information

1
National Center for Advancing Translational Sciences, National Institutes of Health , Bethesda, Maryland 20892, United States.
2
Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health , Bethesda, Maryland 20892, United States.
3
Department of Biology, Loyola University Chicago , Chicago, Illinois 60660, United States.
4
Microbiology and Immunology Department, Uniformed Services University of the Health Sciences , 4301 Jones Bridge Road, Bethesda, Maryland 20814, United States.

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.

KEYWORDS:

Torin; benzo[h][1,6]naphthyridin-2(1H)-ones; gametocytocidal activity; malaria; one-pot reaction; quinoline

PMID:
29024590
PMCID:
PMC5870878
DOI:
10.1021/acscombsci.7b00119
[Indexed for MEDLINE]
Free PMC Article

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