Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties |
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| Authors: | Auvin Serge Auguet Michel Navet Edith Harnett Jeremiah J Viossat Isabelle Schulz Jocelyne Bigg Dennis Chabrier Pierre E |
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| Affiliation: | Department of Medicinal Chemistry, Beaufour-Ipsen Research Laboratories, Institut Henri Beaufour, 5, Avenue du Canada, 91966 Les Ulis Cedex, France. serge.auvin@beaufour-ipsen.com |
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| 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 (IC(50)=0.12 microM) and lipid peroxidation (IC(50)=0.4 microM) 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. |
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