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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates
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Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates

机译:新型抗炎活性美沙拉嗪-甲硝唑偶联物的合成及QSAR研究

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摘要

Novel, mesalazine, metronidazole conjugates 6a-e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties. (C) 2015 Elsevier Ltd. All rights reserved.
机译:利用苯并三唑化学合成了具有氨基酸接头的新型美沙拉嗪,甲硝唑共轭物6a-e。所有新型双结合物的生物学数据均显示:(a)一些双结合物具有与母体药物相当的抗炎活性;(b)有效的双结合物未见可见的胃部病变。 3D-药效团和2D-QSAR建模支持观察到的生物特性。 (C)2015 Elsevier Ltd.保留所有权利。

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