Structure-Bioactivity Relationships of Lapatinib Derived Analogs Against Schistosoma mansoni

ACS Medicinal Chemistry Letters(2020)

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摘要
We recently reported a series of compounds for a solubility-driven optimization campaign of anti-trypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, Schistosoma mansoni. This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization.
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关键词
Schistosomiasis,Schistosoma spp,Target class repurposing,Neglected tropical disease,Parasite-hopping
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