521098-12-4Relevant academic research and scientific papers
Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties.
Auvin, Serge,Auguet, Michel,Navet, Edith,Harnett, Jeremiah J,Viossat, Isabelle,Schulz, Jocelyne,Bigg, Dennis,Chabrier, Pierre E
, p. 209 - 212 (2003)
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.
4-ARYL- AND 4-ARYLTHIO-5-HYDROXY-2(5H)-FURANONES AS INHIBITORS OF PHOSPHOLIPASE A2
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, (2008/06/13)
The invention provides novel 5-hydroxy-4-aryl- and 5-hy-droxy-4-(arylthio)-2(5H)-furanones of the following structure: wherein R contains from about five to about twenty carbon atoms and is defined herein; X is oxygen, sulfur, S02, NH, N(lower alkyl), N(lower acyl), aminocarbonyl, carbonyl, carbonylamino, CH2 or a carbon-carbon bond; Y is hydrogen, halogen, lower alkyl, nitro, alkylthio, perfluoroalkyl, hydroxy, or lower alkoxy(C1-C8); Z is sulfur or a carbon-carbon bond; and Q is H, an alkyl of from 1-20 carbon atoms, COR', COOR', CONHR', PO(OR')2, PO(OR')R" wherein R' and R" are independently selected from the group consisting of H, an alkyl of from 1-20 carbon atoms, phenyl, and substituted phenyl and prodrugs thereof and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising these compounds, methods of using these compounds as inhibitors of inflammation and for treating other diseases characterized by the overproduction of arachidonic acid metabolites, intermediates and methods of preparing these compounds are also provided.
