Author/Authors :
Serge Auvin، نويسنده , , Michel Auguet، نويسنده , , Edith Navet، نويسنده , , Jeremiah J. Harnett، نويسنده , , Isabelle Viossat، نويسنده , , Jocelyne Schulz، نويسنده , , Dennis Bigg، نويسنده , , Pierre-E. Chabrier، نويسنده ,
Abstract :
A series of hybrid compounds possessing an nNOS pharmacophore linked to an antioxidant fragment has been synthesized. Among them, compound 8d, a propofol derivative, displayed the greatest dual potencies against nNOS (IC50=0.12 μM) and lipid peroxidation (IC50=0.4 μM) accompanied with e/nNOS selectivity (67.5). This shows that nNOS was able to accommodate very bulky groups such as di-tert-butyl or di-iso-propyl phenol in its active site.
