PMID: 15248458Jul 14, 2004Paper

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

Die Pharmazie
K GörlitzerJ Wiesner

Abstract

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.

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