Novel lead structures for antimalarial farnesyltransferase inhibitors

Through the combination of nitrophenylfurylacryloyl moiety which has been designed to occupy an aryl binding site of farnesyltransferase with several AA(X)-peptidomimetic substructures some novel farnesyltransferase inhibitors were obtained. Evaluation of their antimalarial activity and some initial...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Pharmazie 2005-05, Vol.60 (5), p.323-327
Hauptverfasser:	Kettler, K., Sakowski, J., Wiesner, J., Ortmann, R., Jomaa, H., Schlitzer, M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkyl and Aryl Transferases - antagonists & inhibitors Alkyl and Aryl Transferases - biosynthesis Amines - chemical synthesis Amines - pharmacology Animals Antimalarials - chemical synthesis Antimalarials - pharmacology Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Farnesyltranstransferase Magnetic Resonance Spectroscopy Nitro Compounds - chemical synthesis Nitro Compounds - pharmacology Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Plasmodium falciparum - growth & development Saccharomyces cerevisiae - enzymology
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	Through the combination of nitrophenylfurylacryloyl moiety which has been designed to occupy an aryl binding site of farnesyltransferase with several AA(X)-peptidomimetic substructures some novel farnesyltransferase inhibitors were obtained. Evaluation of their antimalarial activity and some initial modifications yielded a 4-benzophenone- and a sulfonamid-based novel lead for antimalarial farnesyltransferase inhibitors.
ISSN:	0031-7144