13‐[(N‐Alkylamino)methyl]‐8‐oxodihydrocoptisines were synthesized to evaluate antibacterial activity against Clostridium difficile and activating x‐box‐binding protein 1 (XBP1) activity, biological properties both associated with ulcerative colitis. Improving structural stability and ameliorating biological activity were major concerns. Different substituents on the structural modification site were involved to explore the influence of diverse structures on the bioactivities. The target compounds exhibited the desired activities with definite structure–activity relationship. In the series of 13‐[(N‐n‐alkylamino)methyl]‐8‐oxodihydrocoptisines, the length of n‐alkyl groups has a definite effect on the bioactivity, elongation of the length increasing the antibacterial activity. The synthesized compounds were determined to display strong or weak XBP1‐activating activity in vitro. The preliminary results of this study warrant further medicinal chemistry studies on these synthesized compounds.

中文翻译：

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13-(N-烷基)-氨基甲基-8-氧代二氢黄连素对艰难梭菌的抗菌活性和XBP1活化特性的合成和构效关系

合成 13-[(N-Alkylamino)methyl]-8-oxodihydrocoptisines 以评估对艰难梭菌的抗菌活性和激活 x-box 结合蛋白 1 (XBP1) 活性，两者都与溃疡性结肠炎相关的生物学特性。提高结构稳定性和改善生物活性是主要关注点。涉及结构修饰位点上的不同取代基，以探索不同结构对生物活性的影响。目标化合物表现出所需的活性，具有明确的构效关系。在13-[(N-n-烷基氨基)甲基]-8-氧代二氢黄连素系列中，n-烷基的长度对生物活性有一定的影响，长度的延长增加了抗菌活性。合成的化合物被确定在体外显示出强或弱的 XBP1 激活活性。这项研究的初步结果需要对这些合成化合物进行进一步的药物化学研究。