Enhanced water-soluble derivative of PC407 as a novel potential COX-2 inhibitor injectable formulation |
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| Affiliation: | 1. Department of Chemistry, University of the Pacific, 3601 Pacific Avenue, Stockton, CA 95211, USA;2. Department of Chemistry, Yeshiva University, 2495 Amsterdam Avenue, New York, NY 10033, USA;1. Department of Mechanical Engineering and Engineering Science, University of North Carolina at Charlotte, Charlotte, NC, USA;2. Global Engineering & Materials, Inc., Princeton, NJ, USA;3. Department of Civil, Environmental and Architectural Engineering, University of Colorado at Boulder, Boulder, CO, USA;1. Departamento de Química Fundamental, Universidade da Coruña, E-15008 La Coruña, Spain;2. Departamento de Química Inorgánica, Universidad de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;1. College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 34134, Republic of Korea;2. College of Pharmacy, Chungbuk National University, Cheongju 19421, Republic of Korea |
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| Abstract: | PC407 is an effective COX-2 inhibitor in non-steroidal anti-inflammatory drug development but the poor solubility limits their usefulness. The aim of the study was to prepare and evaluate 4-oxo-4-[4-(5-(naphthalen-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamido]butyrate disodium, a derivative of PC407 with enhanced water solubility for injectable formulation. The prepared derivative displayed interesting high aqueous solubility (20.3 mg/mL, much superior to the parent compound PC407, 1.6 μg/mL) with confirmed in vivo analgesic activity. This derivative represents the profiles of prodrug and potential candidate of PC407 for the development of injectable COX-2 inhibitor due to extraordinary water solubility, low toxicity, and impressive analgesic activity. |
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| Keywords: | COX-2 inhibitor Prodrug Solubility Injectable formulation |
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