On the inhibitory potency of imidazole and its derivatives on thromboxane synthetase

The relative inhibitory potency of imidazole and derivatives on thromboxane synthetase from human platelets was found to be increased by substitution of the 1-position and abolished in other positions. The potency of 1-substituted imidazoles was increased as the side chain became more hydrophobic. A...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Biochemical and biophysical research communications 1978-01, Vol.80 (1), p.236-242
Hauptverfasser: Tai, Hsin-Hsiung, Yuan, Barbara
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The relative inhibitory potency of imidazole and derivatives on thromboxane synthetase from human platelets was found to be increased by substitution of the 1-position and abolished in other positions. The potency of 1-substituted imidazoles was increased as the side chain became more hydrophobic. Among the imidazole derivatives tested 1-nonyl-imidazole and 1-(2-isopropyl phenyl)-imidazole showed the highest potency with I 50 in the range of 10 −8 M. Inhibition by imidazole and its derivatives appeared to be very specific for thromboxane synthetase since other enzymes in prostaglandin endoperoxide metabolism were not affected. Kinetic studies indicated that inhibition was competitive with respect to prostaglandin endoperoxide substrate.
ISSN:0006-291X
1090-2104
DOI:10.1016/0006-291X(78)91128-2