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2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites |
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| Authors: | Heinrich Swetlana Altenkämper Mirko Bechem Benjamin Perruchon Johann Ortmann Regina Dahse Hans-Martin Wang Yulin Lanzer Michael Schlitzer Martin |
| Affiliation: | a Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, Marburg 35032, Germany b Leibniz-Institut für Naturstoff-Forschung und Infektionsbiologie e. V. Hans-Knöll-Institut, Beutenbergstrasse 11a, 07745 Jena, Germany c Institut für Parasitologie, Universität Heidelberg, Im Neuenheimer feld 24, Heidelberg 69120, Germany |
| Abstract: | 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. |
| Keywords: | Antimalarial agents Plasmodium falciparum Benzophenone derivatives QSAR Enhanced selectivity |
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