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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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Supplementary files

Article information


Submitted
24 mar. 2015
Accepted
06 maí 2015
First published
06 maí 2015

Med. Chem. Commun., 2015,6, 1173-1177
Article type
Concise Article
Author version available

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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