Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371917 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Only a few COX-1-selective inhibitors are currently available, and the research on COX-1 selective inhibitors is not fully developed. The authors have produced several COX-1 selective inhibitors including N-(5-amino-2-pyridinyl)-4-trifluoromethylbenzamide: TFAP (3). Although 3 shows potent analgesic effect without gastric damage, the urine after administration of 3 becomes red-purple. Since the colored-urine should be avoided for clinical use, in this research we examined the cause of the colored-urine. UV-vis spectra and LC-MS/MS analyses of urine samples and metabolite candidates of 3 were performed to afford information that the main reason of the colored urine is a diaminopyridine (4), produced by metabolization of 3. This information is useful to design new COX-1 selective inhibitors without colored urine based on the chemical structure of 3.
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Authors
Hiroki Kakuta, Ryosuke Fukai, Zheng Xiaoxia, Fuminori Ohsawa, Takeshi Bamba, Kazumasa Hirata, Akihiro Tai,