Zheng Shaojun, Zhou Xinping, Xu Shixun, Zhu Rui, Bai Hongjin, Zhang Jiwen
School of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang 212003, Jiangsu, China.
Key Laboratory of Protection & Utilization of Biological Resources in Tarim Basin of Xinjiang Production and Construction Corps/College of Life Sciences, Tarim University, Alar 843300, Xinjiang, China.
Molecules. 2016 Sep 9;21(9):1207. doi: 10.3390/molecules21091207.
A total of 29 novel tetrahydropyrroloindol-based calycanthaceous alkaloid derivatives were synthesized from indole-3-acetonitrile in good yields. The synthesized compounds were evaluated against nine strains of bacteria and a wide range of plant pathogen fungi. Bioassay results revealed that majority of the compounds displayed similar or higher in vitro antimicrobial activities than the positive control. The biological activities also indicated that substituents at R₄ and R₅ significantly affect the activities. Notably, compound c4 was found to be most active among the tested calycanthaceous analogues and might be a novel potential leading compound for further development as an antifungal agent. The results could pave the way for further design and structural modification of calycanthaceous alkaloids as antimicrobial agents.
以吲哚 - 3 - 乙腈为原料，高产率地合成了总共29种新型基于四氢吡咯并吲哚的蜡梅科生物碱衍生物。对合成的化合物针对9种细菌菌株和多种植物病原真菌进行了评估。生物测定结果表明，大多数化合物表现出与阳性对照相似或更高的体外抗菌活性。生物活性还表明，R₄和R₅处的取代基显著影响活性。值得注意的是，化合物c4在所测试的蜡梅科类似物中被发现活性最高，可能是一种新型的潜在先导化合物，可进一步开发为抗真菌剂。这些结果可为蜡梅科生物碱作为抗菌剂的进一步设计和结构修饰铺平道路。
