881658-92-0Relevant articles and documents
Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria
Kandepedu, Nishanth,Gonzàlez Cabrera, Diego,Eedubilli, Srinivas,Taylor, Dale,Brunschwig, Christel,Gibhard, Liezl,Njoroge, Mathew,Lawrence, Nina,Paquet, Tanya,Eyermann, Charles J.,Spangenberg, Thomas,Basarab, Gregory S.,Street, Leslie J.,Chibale, Kelly
, p. 5692 - 5703 (2018/06/19)
A novel 2,8-disubstituted-1,5-naphthyridine hit compound stemming from the open access Medicines for Malaria Venture Pathogen Box formed a basis for a hit-to-lead medicinal chemistry program. Structure-activity relationship investigations resulted in compounds with potent antiplasmodial activity against both chloroquine sensitive (NF54) and multidrug resistant (K1) strains of the human malaria parasite Plasmodium falciparum. In the humanized P. falciparum mouse efficacy model, one of the frontrunner compounds showed in vivo efficacy at an oral dose of 4 × 50 mg·kg-1. In vitro mode-of-action studies revealed Plasmodium falciparum phosphatidylinositol-4-kinase as the target.
NAPHTHYRIDIN-2 (1 H)-ONE COMPOUNDS USEFUL AS ANTIBACTERIALS
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Page/Page column 17-18, (2010/08/08)
Compounds of Formula (I) wherein substituents R1, R2 and R5 are as defined, and Ar represents substituted phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, furanyl, imidazolyl and thiophenyl substituted by a hydroxyalkyl substituent and an optional other substituent; compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
Compounds
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Page/Page column 15, (2009/08/14)
Compounds of Formula (I), compositions containing them, their use in therapy, including their use as antibacterials, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.