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pubmed-article:11844668pubmed:abstractTextWe have described 5-(4-propoxycinnamoylamino)-2-(4-tolylacetylamino)benzophenone 6e as a novel lead for anti-malarial agents. Anti-malarial activity of these 5-(4-propoxycinnamoylamino)benzophenones proved to be quite sensitive against variations of the acyl substituent at the 2-amino group. Best activity was obtained with phenylacetic acid moieties carrying small substituents in the para-position. From the para-substituents evaluated, the trifluoromethyl group yielded the most active compound (6j) in this series (IC50=120 nM). Deviations from the phenylacetic acid substructure, shifting the substituent into the ortho-position or bulkier para-substituents resulted in a significant reduction in anti-malarial activity.lld:pubmed
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pubmed-article:11844668pubmed:articleTitleStructure-activity relationships of novel anti-malarial agents. Part 3: N-(4-acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides.lld:pubmed
pubmed-article:11844668pubmed:affiliationBiochemisches Institut der Universitatsklinik Giessen, Friedrichstrasse 24, D-35249, Giessen, Germany.lld:pubmed
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