Bioorganic & Medicinal Chemistry Letters 2003-02-10

Structure-activity relationships of novel anti-malarial agents: part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.

Jochen Wiesner, Katja Kettler, Jacek Sakowski, Regina Ortmann, Hassan Jomaa, Martin Schlitzer

Index: Bioorg. Med. Chem. Lett. 13(3) , 361-3, (2003)

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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.