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Synthesis, characterization and biological evaluation of naproxen Cu(II) complexes

Journal 2018 · IF 2.011 · 发表于 2018 年 10 月 22 日
作者: Yi-Chun Chu,Tian-Tian Wang,Xiang-Yu Ge,Peng-Hao Yang,Wei Li,Jing Zhao,Hai-Liang Zhu
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摘要

Two Cu(II) complexes of the non-steroidal anti-inflammatory drug Naproxen were synthesized, characterized and evaluated for anti-inflammatory, analgesic, ulcerogenic and urease inhibition activities. The complex 1 [Cu(nap) 2 (H 2 O) 3 ]·H 2 O was reported previously, and the crystal structure of complex 2 [Cu(nap) 2 (dap)(H 2 O)] (nap = Naproxen, dap = 1,3-diaminopropane) was confirmed by X-ray diffraction crystallography . The anti-inflammatory and ulcerogenic study showed that the compounds 1 and 2 were the promising anti-inflammatory agents and demonstrated significant gastric tolerance when compared with Naproxen, especially for complex 1 with the edema inhibition of 93.6% after 3 h, and ulcer index of 15 ± 2. Analgesic and urease inhibition assay showed that complex 2 was a potent urease inhibitor with the IC 50 value of 1.69 ± 0.08  μ M and pain inhibition value of 65%. As effective urease inhibitors, molecular docking study was performed to investigate the binding mode of the complexes with urease.