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Issue 10, 2014
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A critical evaluation of pyrrolo[2,3-d]pyrimidine-4-amines as Plasmodium falciparum apical membrane antigen 1 (AMA1) inhibitors

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Abstract

We have determined that a previously reported class of pyrrolo[2,3-d]pyrimidine-4-amines exhibit low binding to apical membrane antigen 1 (AMA1) and suffer from unattractive qualities, such as aggregation. We attempted to remove these traits by generating molecules with improved solubility, but this did not translate into enhanced binding affinity or inhibition of parasite growth in erythrocytes. These results indicate that anti-malarial activity is not primarily due to inhibition of AMA1 function, but mediated by an alternate or additional mechanism of action.

Graphical abstract: A critical evaluation of pyrrolo[2,3-d]pyrimidine-4-amines as Plasmodium falciparum apical membrane antigen 1 (AMA1) inhibitors

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Publication details

The article was received on 28 Feb 2014, accepted on 23 Jul 2014 and first published on 23 Jul 2014


Article type: Concise Article
DOI: 10.1039/C4MD00090K
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Med. Chem. Commun., 2014,5, 1500-1506

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    A critical evaluation of pyrrolo[2,3-d]pyrimidine-4-amines as Plasmodium falciparum apical membrane antigen 1 (AMA1) inhibitors

    S. M. Devine, S. S. Lim, I. R. Chandrashekaran, C. A. MacRaild, D. R. Drew, C. O. Debono, R. Lam, R. F. Anders, J. G. Beeson, M. J. Scanlon, P. J. Scammells and R. S. Norton, Med. Chem. Commun., 2014, 5, 1500
    DOI: 10.1039/C4MD00090K

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