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Issue 6, 2015
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Discovery of oxybisbenzoylamides as a new class of antimalarial agents

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Abstract

We have previously described several potent dual inhibitors of Plasmodium falciparum (Pf) growth characterized by the presence of statine, a β-hydroxyl amino acid able to inhibit parasite's plasmepsins (PLMs). While investigating the mechanism of action of these inhibitors, new compounds derived from statine were synthesized, which lost the ability to inhibit PLMs, but retained a significant Pf growth inhibition. Further structural simplifications showed that the inhibition of Pf viability was ascribed to a new pharmacophore never described before as antimalarial.

Graphical abstract: Discovery of oxybisbenzoylamides as a new class of antimalarial agents

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Publication details

The article was received on 24 Mar 2015, accepted on 06 May 2015 and first published on 06 May 2015


Article type: Concise Article
DOI: 10.1039/C5MD00115C
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Med. Chem. Commun., 2015,6, 1173-1177

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    Discovery of oxybisbenzoylamides as a new class of antimalarial agents

    A. Pancotti, S. Parapini, M. Dell'Agli, L. Gambini, C. Galli, E. Sangiovanni, N. Basilico, E. Bosisio, D. Taramelli and S. Romeo, Med. Chem. Commun., 2015, 6, 1173
    DOI: 10.1039/C5MD00115C

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