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Die Kinase PfCLK3 spielt eine entscheidende Rolle bei der Regulation des RNA-Splicing von Malariaparasiten und ist essentiell für das Überleben des Blutstadiums Plasmodium falciparum. Wir haben kürzlich Pf CLK3 als Wirkstoffziel bei Malaria validiert, das prophylaktisches, übertragungsblockierendes und heilendes Potenzial bietet. Hier beschreiben wir die Synthese unseres ersten Treffers TCMDC-135051 1 und die Bemühungen, einen SAR mit einer 7-Azaindol-basierten Serie zu etablieren. Insgesamt 14 Analoga wurden in einem TR-FRET-Assay gegen die vollständige rekombinante Proteinkinase PfCLK3 und 10 weitere in Parasiten 3D7 (chloroquinempfindlichen) Stämmen von P. falciparum untersucht. SAR in Bezug auf die Ringe A und B wurde festgelegt. Diese Daten legen nahe, dass TCMDC-135051 1eine vielversprechende Leitsubstanz für die Entwicklung neuer Malariamedikamente mit einem neuartigen Wirkmechanismus ist, der auf Pf CLK3 abzielt.

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