Bicyclic Pyrrolidine Inhibitors of Toxoplasma gondii Phenylalanine t-RNA Synthetase with Antiparasitic Potency In Vitro and Brain Exposure
Chloe C. Ence,
Taher Uddin,
Julien Borrel
et al.
Abstract:Previous studies have shown that bicyclic azetidines
are potent
and selective inhibitors of apicomplexan phenylalanine tRNA synthetase
(PheRS), leading to parasite growth inhibition in vitro and in vivo,
including in models of Toxoplasma infection. Despite
these useful properties, additional optimization is required for the
development of efficacious treatments of toxoplasmosis from this inhibitor
series, in particular, to achieve optimal exposure in the brain. Here,
we describe a series of PheRS inhibitors bu… Show more
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