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Antimalarial and antitrypanosomal activity of a series of amide and sulfonamide derivatives of a 2,5-diaminobenzophenone |
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| Authors: | Mirko Altenkämper Benjamin Bechem Johann Perruchon Swetlana Heinrich Andrea Mädel Regina Ortmann Hans-Martin Dahse Ellen Freunscht Yulin Wang Jennifer Rath August Stich Manuela Hitzler Peter Chiba Michael Lanzer Martin Schlitzer |
| Institution: | 1. Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, 35032 Marburg, Germany;2. Leibniz-Institut für Naturstoff-Forschung und Infektionsbiologie e.V. Hans-Knöll-Institut, Beutenbergstrasse 11a, 07745 Jena, Germany;3. Institut für Parastitologie, Universität Heidelberg, Im Neuenheimer Feld 24, 69120 Heidelberg, Germany;4. Tropenmedizinische Abteilung, Missionsärztliche Klinik GmbH, Salvatorstr. 7, 97074 Würzburg, Germany;5. Center for Physiology, Pathophysiology and Immunology, Institute of Medical Chemistry, Medical University of Vienna, Austria |
| Abstract: | Here, we describe a series of readily obtainable benzophenone derivatives with antimalarial and antitrypanosomal activity. The most active compounds display submicromolar activity against Plasmodium falciparum. Micromolar activity is obtained against Trypanosoma brucei. Main problem of the compounds is low selectivity. However, there are indications that separation of antimalarial and cytotoxic activity might by possible. In addition, some compounds inhibit human ABC transporter with nanomolar activity. |
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