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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >Synthesis, Biological Activity of 2-phenylindolizine Acetamide Derivatives as Potential Antibacterial Agents
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Synthesis, Biological Activity of 2-phenylindolizine Acetamide Derivatives as Potential Antibacterial Agents

机译：2-苯基吲哚嗪乙酰胺衍生物作为潜在抗菌剂的合成，生物活性

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The discovery of camptothecin and its analogs was the major breakthrough through which ‘‘indolizine moiety’’ came into limelight. A novel compounds, 2-phenylindolizine acetamide derivatives (8a-8k) has been synthesized by the reaction of 2-oxo-2-(2-phenylindolizin-3-yl)acetyl chloride (6) with different aromatic compounds (7a-7k) in presence of triethylamine in Dichloromethane (DCM). The synthesis and screened for their antimicrobial activities of novel class of 2-phenylindolizin acetamide scaffolds are described by variation in therapeutic effects of parent molecule. Result revealed that the target compounds 8b, 8a and 8f exhibited a remarkable increase of antimicrobial activity against than reference compound ampicillin, fluconazole against in three medically relevant organisms like Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa is observed. Further, 8j and 8d showed better activity against antifungal strains Candida albicans, Aspergillus flavus and Aspergillus fumigates.
机译：喜树碱及其类似物的发现是“吲哚嗪部分”的重大突破。通过2-氧代-2-（2-苯基吲哚嗪-3-基）乙酰氯（6）与不同芳族化合物（7a-7k）的反应合成了一种新型化合物2-苯基吲哚嗪乙酰胺衍生物（8a-8k）。在三乙胺的二氯甲烷（DCM）溶液中。通过改变母体分子的治疗作用来描述新型的2-苯基吲哚嗪乙酰胺支架的合成及其抗菌活性。结果表明，在三种医学相关生物如金黄色葡萄球菌，大肠杆菌，铜绿假单胞菌中，目标化合物8b，8a和8f的抗微生物活性比参考化合物氨苄西林，氟康唑显着提高。此外，8j和8d表现出更好的抗真菌菌株白色念珠菌，黄曲霉和熏蒸曲霉的活性。

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