Optimization of 2,8-Diaryl-1,5-naphthyridines as Plasmodium falciparum Phosphatidylinositol 4‑Kinase Inhibitors with Improved ADME Profiles and In Vivo Efficacy

Previously reported antimalarial Plasmodium phosphatidylinositol 4-kinase IIIβ 2,8-diaryl-1,5-naphthyridine inhibitors have shown suboptimal physicochemical and pharmacokinetic properties. A focused target-based structure–activity relationship and structure–property optimization studies identified s...

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المؤلف الرئيسي:	Godwin A. Dziwornu (22057544) (author)
مؤلفون آخرون:	Donald Seanego (18881995) (author), Stephen Fienberg (4710014) (author), Venkata S. Sypu (18881998) (author), Nicolaas Salomane (18882013) (author), Liezl Krugmann (21343901) (author), Dale Taylor (1463830) (author), Keabetswe Masike (3905104) (author), Mathew Njoroge (1463821) (author), Nonlawat Boonyalai (6053441) (author), Marcus C. S. Lee (7553543) (author), Luiz C. Godoy (614562) (author), Charisse Flerida Pasaje (9353757) (author), Jacquin C. Niles (304325) (author), Gregory S. Basarab (1550479) (author), Lauren B. Coulson (18882022) (author), Sandeep R. Ghorpade (1786699) (author), Kelly Chibale (503778) (author)
منشور في:	2025
الموضوعات:	Biochemistry Cell Biology Genetics Molecular Biology Physiology Pharmacology Sociology Immunology Cancer Infectious Diseases Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified Physical Sciences not elsewhere classified shows low selectivity shown suboptimal physicochemical plasmodium falciparum malaria pi4kβ ); however kg qd doses improved adme profiles humanized nod -< herg channel inhibition improved physicochemical properties improved pharmacokinetic profile new frontrunner compound kinase iiiβ 2 27 </ b pharmacokinetic properties 2rγnull </ scid il reduced parasitaemia naphthyridine inhibitors mouse model map4k4 kinases mammalian cytotoxicity human mink1 high concentrations good target focused target cell activities
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Optimization of 2,8-Diaryl-1,5-naphthyridines as Plasmodium falciparum Phosphatidylinositol 4‑Kinase Inhibitors with Improved ADME Profiles and In Vivo Efficacy

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