Novel Azulenyl Nitrone Spin Trapping Agents – IP 1101

Spin trapping agents have been widely used for freed radicalresearch and therapeutic applications. The superoxide radical is considered toplay important roles in physiological processes as well as in the genesis ofdiverse cytotoxic conditions such as cancer, various cardiovascular disordersand neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS),Parkinson’s disease (PD) and Alzheimer’s Disease (AD). The detection andquantification of superoxide within cells is of critical importance tounderstand biological roles of superoxide and to develop preventive strategiesagainst free radical-mediated diseases. Cyclic nitrone spin traps such as DMPO, EMPO, DEPMPO, BMPOand their derivatives have been widely used in conjunction with ESRspectroscopy for the detection of cellular superoxide with some success.However, the formation of unstable superoxide adducts from the reaction ofcyclic nitrones with superoxide is a stumbling block in detecting superoxide byusing Electron Spin Resonance (ESR). The compounds of this invention can trap superoxideefficiently yielding UV-Visible products and even potentially fluorescence-detectableorange products. Hence, the chromotropic detection of superoxide using thesecompounds provides an improved method for free superoxide radical detection. Anne Laure Schmitt Olivier 305-348-5948

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