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Open Access [1]Benzofuro[3,2-b]pyridin-4-yl-amine – Synthese und Prüfung auf Wirksamkeit gegen Malaria

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Der 4-Chlorbenzofuro[3,2-b]pyridin-3-carbonsäureethylester (2) reagierte mit den Hydrochloriden der Mono- und Bis-Phenol-Mannich-Basen 3 zu den Amodiaquin- und Pyronaridin-Analogen 4. Die Umsetzung von 2 mit der Novaldiamin-Base (5) in einer Phenolschmelze lieferte das Chloroquin-Analoge 6. Die aktivste Substanz 4c hemmte das Wachstum des Malaria-Parasiten Plasmodium falciparum mit einer IC50 von 500 nM.

[1]Benzofuro[3,2-b]pyridin-4-yl-amines – synthesis and investigation of activity against malaria

The ethyl 4-chlorobenzofuro[3,2-b]pyridine-3-carboxylate (2) reacted with the hydrochlorides of the mono- and bis-phenol Mannich bases 3 to yield the amodiaquine and pyronaridine analogues 4. The chloroquine analogue 6 was formed by melting 2 with the novaldiamine base (5) in phenol. The most active compound 4c inhibited the growth of the malaria parasite Plasmodium falciparum with an IC50 of 500 nM.

Document Type: Research Article

Affiliations: 1: Institut für Pharmazeutische Chemie der Technischen Universität Braunschweig, Beethovenstraße 55, Braunschweig, D-38106, Germany, Email: 2: Institut für Pharmazeutische Chemie der Technischen Universität Braunschweig, Braunschweig, Germany 3: Biochemisches Institut der Universitätsklinik Gießen, Gießen, Germany

Publication date: 2004-06-01

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