Abstract:We discovered dibenzannulated medium-ring keto lactams
(11,12-dihydro-5H-dibenzo[b,g]azonine-6,13-diones)
as a new antimalarial chemotype. Most of these had chromatographic
LogD7.4 values ranging from <0 to 3 and good kinetic
solubilities (12.5 to >100 μg/mL at pH 6.5). The more polar
compounds in the series (LogD7.4 values of <2) had the
best metabolic stability (CLint values of <50 μL/min/mg
protein in human liver microsomes). Most of the compounds had relatively
low cytotoxicity, with IC50 values >30 μM, … Show more
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