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2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites

Previously we described a series of 5-acylaminobenzophenones with considerable antimalarial activity. Unfortunately, most compounds also displayed high cytotoxicity resulting in low selectivity towards malaria parasites. Through the replacement of the 5-acylamino moiety by simple chlorine and furthe...

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Main Authors: Heinrich, Swetlana (Author) , Altenkämper, Mirko (Author) , Bechem, Benjamin (Author) , Perruchon, Johann (Author) , Ortmann, Regina (Author) , Dahse, Hans-Martin (Author) , Wang, Yulin (Author) , Lanzer, Michael (Author) , Schlitzer, Martin (Author)
Format: Article (Journal)
Language:English
Published: [April 2011]
In: European journal of medicinal chemistry
Year: 2011, Volume: 46, Issue: 4, Pages: 1331-1342
ISSN:1768-3254
DOI:10.1016/j.ejmech.2011.01.056
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/j.ejmech.2011.01.056
Verlag, lizenzpflichtig, Volltext: https://www.sciencedirect.com/science/article/pii/S022352341100078X
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Author Notes:Swetlana Heinrich, Mirko Altenkämper, Benjamin Bechem, Johann Perruchon, Regina Ortmann, Hans-Martin Dahse, Yulin Wang, Michael Lanzer, Martin Schlitzer
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Summary:Previously we described a series of 5-acylaminobenzophenones with considerable antimalarial activity. Unfortunately, most compounds also displayed high cytotoxicity resulting in low selectivity towards malaria parasites. Through the replacement of the 5-acylamino moiety by simple chlorine and further modifications of the 2-acylamino residue we could obtain inhibitors with improved selectivity towards malaria parasites combined with an acceptable reduction of antimalarial activity.
Item Description:Available online 3 February 2011
Gesehen am 04.10.2022
Physical Description:Online Resource
ISSN:1768-3254
DOI:10.1016/j.ejmech.2011.01.056

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