Skip to main content

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

Download Article:
 Download
(PDF 88.6943359375 kb)
 

Abstract:

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: k.goerlitzer@tu-bs.de 2: Institut für Pharmazeutische Chemie der Technischen Universität Braunschweig, Braunschweig, Germany 3: Biochemisches Institut der Universitätsklinik Gießen, Gießen, Germany

Publication date: 2004-06-01

More about this publication?
  • Pharmazie is a leading journal in the field of pharmaceutical sciences. As a peer-reviewed scientific journal, Pharmazie is regularly indexed in the relevant databases like Web of science, Journal Citation Reports and many others. The journal is open for submissions from the whole spectrum of pharnaceutical sciences including Pharmaceutical Chemistry, Experimental and Clinical Pharmacology, Drug Analysis, Pharmaceutics, Pharmaceutical Biology, Clinical Pharmacy etc.
  • Information for Authors
  • Submit a Paper
  • Subscribe to this Title
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
X
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more