Article

1,3-diphenylureido hydroxamate: a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors

2023-08-28

Abstract excerpt

We report a series of 1,3-diphenylureido hydroxamate HDAC inhibitors evaluated against sensitive and drug-resistant P. falciparum strains. Compounds 8a-d show potent antiplasmodial activity, indicating that a phenyl spacer allows improved potency relative to cinnamyl and di-hydrocinnamyl linkers. In vitro , mechanistic studies demonstrated target activity for Pf HDAC1 on a recombinant level, which agreed with cell...

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Literature Corpus work: 0d3199d4-208a-5855-b434-f11767906928
DOI: 10.21203/rs.3.rs-3272060/v1

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