Synthesis,hepatotoxic evaluation and antipyretic activity of nitrate ester analogs of the acetaminophen derivative SCP-1 |
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| Authors: | Madhurima Das Surjyadipta Bhattacharjee Frank R Fronczek Nicolas G Bazan Mark L Trudell |
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| Institution: | 1. Department of Chemistry, University of New Orleans, New Orleans, LA 71048 USA;2. Neuroscience Center of Excellence, Louisiana State University Health Science Center, New Orleans, LA 70112, USA;3. Department of Chemistry, Louisiana State University, Baton Rouge, LA 70803, USA |
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| Abstract: | A series of nitrate ester analogues of the acetaminophen derivative SCP-1 were prepared by triflic acid catalyzed O-acylation of SCP-1 with chloroalkanoyl chlorides followed by nitration with silver nitrate. The chloroesters and corresponding nitrate esters were obtained in high yields. Preliminary hepatotoxicity studies revealed nitrate esters 5b (MD-38) and 5c (MD-39) to be well tolerated by human hepatocytes and had little effect on the three cytochrome P450 enzymes tested (CYP3A4, CYP2E1 and CYP2D6). In addition, the nitrate ester 5c (MD-39) exhibited antipyretic activity similar to acetaminophen. |
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| Keywords: | Nitrate ester NO donor Hepatotoxicity Antipyretic activity Acetaminophen |
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