ORGN 370 |
Site-specific aminoglycoside derivatives for use in Fluorescence Polarization Immunoassays
| Mitali Ghoshal, Gerald Sigler, Jane Tsai, Joyce Chang, Cheryl Brenner, Thomas Steppe, Salvatore J. Salamone, and Joseph Passarelli. Roche Diagnostics Corporation, 9115 Hague Road, Indianapolis, IN 46250 |
| In Roche's current Fluorescence Polarization Immunoassays (FPIAs) for aminoglycosides, Fluorescence Polarization (FP) tracers are synthesized by reacting unprotected polyamino functionalities of aminoglycosides with appropriate fluorescein reagents. This procedure requires tedious and difficult purification procedures and leads to a problem of lot to lot reproducibility. Metal complexation between the neighboring amino groups and hydroxyl groups of aminoglycosides using bi-valent transition metals is known in the literature [JCS Perkin 1, (1981), 2186-2208)]. We used the above technique of selectively protecting amino groups of aminoglycosides to prepare new site-selective fluorescence polarization (FP) tracers. Fluorescence polarization tracers for amikacin (1) and tobramycin (2 & 3) are described. Using a similar technique the site-selective gentamicin FP tracers (gentamicin C1, C2 and C1a) can also be prepared. These tracers have been used in the Fluorescence Polarization Immunoassays (FPIAs). The syntheses of these FP tracers and the results of their use in the immunoassay will be discussed.  |
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Physical Organic, Materials, Heterocycles, Aromatics, Metal-Mediated Reactions
8:00 PM-10:00 PM, Tuesday, September 9, 2003 Hilton New York -- Americas Hall 1, Poster
Sci-Mix
8:00 PM-10:00 PM, Monday, September 8, 2003 Javits Convention Center -- North Pavillion, Sci-Mix
Division of Organic Chemistry
The 226th ACS National Meeting, New York, NY, September 7-11, 2003
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