Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors |
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Authors: | Shi Lei Li Zi-Lin Yang Ying Zhu Zhen-Wei Zhu Hai-Liang |
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Affiliation: | State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China |
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Abstract: | A series of N-phenylnicotinamides (1-40) were designed and evaluated in vitro for their COX inhibitory activities. Most of the synthesized compounds were proved to be potent and selective inhibitors of COX-1. Compound 28 showed the most potent COX-1 inhibitory activity (COX-1 IC50 = 0.68 ± 0.07 μM) and good selectivity (COX-2 IC50 >100 μM). This compound may be useful as a lead compound for superior COX-1 inhibitors. On the basis of the biological results, structure-activity relationships for the COX-1-inhibitory activities of the synthesized N-phenylnicotinamides were discussed concisely. |
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Keywords: | Cyclooxygenase-1 Inhibitor N-Phenylnicotinamide Structure-activity relationship Molecular docking |
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