Structure-activity relationships of novel anti-malarial agents: part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides |
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Authors: | Wiesner Jochen Kettler Katja Sakowski Jacek Ortmann Regina Jomaa Hassan Schlitzer Martin |
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Institution: | Biochemisches Institut der Universit?tsklinik Giessen, Friedrichstrasse 24, Giessen, Germany. |
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Abstract: | We have developed the 5-(4-nitrophenyl)-2-furyl]acrylic acid substituted benzophenone 4g as a novel lead for anti-malarial agents. Here, we demonstrated that the acyl residue at the 2-amino group of the benzophenone core structure has to be a phenylacetic acid substructure substituted in its para-position with methyl or other substituents of similar size. The trifluoromethyl substituted derivative displayed an IC(50) of 47 nM against the multi-drug resistant Plasmodium falciparum strain Dd2. |
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