Orally Bioavailable Endochin-Like Quinolone Carbonate Ester Prodrug Reduces Toxoplasma gondii Brain Cysts
Author(s) -
J. Stone Doggett,
Tracey L. Schultz,
Alyssa J. Miller,
Igor Bruzual,
Sovitj Pou,
Rolf W. Winter,
Rozalia A. Dodean,
Lev N. Zakharov,
Aaron Nilsen,
Michael K. Riscoe,
Vern B. Carruthers
Publication year - 2020
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.00535-20
Subject(s) - toxoplasma gondii , toxoplasmosis , prodrug , in vitro , pharmacology , biology , adverse effect , quinolone , bioavailability , pyrimethamine , microbiology and biotechnology , immunology , virology , antibiotics , biochemistry , chloroquine , antibody , malaria
Toxoplasmosis is a potentially fatal infection for immunocompromised people and the developing fetus. Current medicines for toxoplasmosis have high rates of adverse effects that interfere with therapeutic and prophylactic regimens. Endochin-like quinolones (ELQs) are potent inhibitors ofToxoplasma gondii proliferationin vitro and in animal models of acute and latent infection. ELQ-316, in particular, was found to be effective orally against acute toxoplasmosis in mice and highly selective forT. gondii cytochromeb over human cytochromeb .
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