Malaria is one of the most important parasitic infectious diseases. It is caused by protozoa of the genus Plasmodium and is transmitted to humans by the bite of a female Anopheles mosquito (vector). The spread of malaria is accompanied by a limited arsenal of effective drugs, emerging drug resistance, severe side effects and lack of availability in the most affected areas. Hence there is an urgent need to develop new antimalarial drugs. The group of Prof. Schlitzer has been working on the development of antimalarial drugs based on a benzophenone-scaffold. Previous work resulted in a 2-acylamino-5-chlorobenzophenone derivative, as lead structure for further optimization. In order to achieve structural modifications systematically the lead compound was formally devided into three molecular regions. These were varied independently and the most active moieties were combined to finally yield more affective antimalarial drugs. Starting from a 2-acylamino-5-chloro-benzophenone derivative it was therefore possible to develop potent amides of
N-acylanthranilic acid, without a detailed knowledge of the molecular target. Classical structural variation combined with biological evaluation in a whole-cell assay led to compounds, which are superior to the lead derivative in terms of activity and selectivity. Along the way, various structural modifications have been evaluated, so that there is now plenty of information on the structure-activity relationship.
Heinrich, Swetlana (1017066345): Entwicklung von N-Acylanthranilsäureamiden als Wirkstoffe gegen P.falciparum. : Philipps-Universität Marburg 2011-12-19. DOI: https://doi.org/10.17192/z2011.0648.
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