Synthesis,potential anti-inflammatory and analgesic activities study of (S)-N-substituted-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamides |
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Authors: | Li-Ping Guan Ya-Nan Xia Qing-Hao Jin Bing-Yu Liu Si-Hong Wang |
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Affiliation: | 1. Food and Pharmacy College, Zhejiang Ocean University Engineering Technology Research Center of Marine Biomedical Products, Zhejiang, Zhoushan 316022, PR China;2. Analysis and Test Center, Yanbian University, Jilin, Yanji 133002, PR China |
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Abstract: | A series of (S)-N-substitued-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives were designed, synthesized and evaluated for their anti-inflammatory and analgesic effects in vivo. Among the synthesized compounds 2a and 2n showed the best anti-inflammatory activity (inhibition rate: 95% and 92.7%, respectively) and analgesic effect (inhibition rate: 100% and 100%, respectively), which was greater than that or nearly equivalent to that of indomethacin. Compounds 2a and 2n were selected to test their inhibitory effects against ovine COX-1 and COX-2 using the cyclooxygenase inhibition assay in vitro. Compounds 2a and 2n are weak inhibitors of COX-1 isozyme but displayed moderate COX-2 isozyme inhibitory effects (IC50 = 0.47 μM and 1.63 μM, respectively) and COX-2 selectivity indexes (SI = 11.5 and 4.8). Furthermore, compound 2a was more inhibitors of COX-2 isozyme active than the reference drug celecoxib. |
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Keywords: | Anti-inflammatory Analgesic COX-1/COX-2 Inhibition assay |
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