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Design, synthesis and biological activity evaluation of novel antibacterial agent (E)-1-(4-chlorobenzyl)-5-styrylindoline-2, 3-dione

机译:(E)-1-(4-氯苄基)-5-styrylindoline-2,3-dione新型抗菌剂的设计,合成及生物活性评价

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摘要

Isatin, an endogenous compound existent in many organisms, shows a wide range of biological activities. In this paper, we like to report the design and synthesis of several isatin derivatives through the acetalization, N-Alkylation, Microwave-asistant Heck coupling reaction and so on. Among those compounds, (E)-1-(4-chlorobenzyl)-5-styryl-indoline-2-carbonyl-3, 3-(ethylenedioxy) dione and (E)-1-(4-chlorob-enzyl)-5-styrylindoline-2, 3-dione possess novel structures and have not been reported before. Five newly synthesized compounds were characterized on the basis of 1H NMR, 13C NMR and mass spectra, and those compounds were tested for their biological activities against Gram+ and Gram− bacteria. Among those compounds, (E)-1-(4-chlorobenzyl)-5-styrylindoline-2, 3-dione demonstrated good antibacterial activity against Escherichia coli (Gram−) and moderate antibacterial activity against Staphyloccocus aureus (Gram+).
机译:Isatin是许多生物中存在的一种内源性化合物,具有广泛的生物活性。在本文中,我们希望通过缩醛化,N-烷基化,微波辅助Heck偶联反应等方法报道几种Isatin衍生物的设计和合成。在这些化合物中,(E)-1-(4-氯苄基)-5-苯乙烯基-二氢吲哚-2-羰基-3、3-(亚乙基二氧基)二酮和(E)-1-(4-氯-烯基)-5 -styrylindoline-2,3-dione具有新颖的结构,以前尚未见报道。根据 1 H NMR, 13 C NMR和质谱对五种新合成的化合物进行了表征,并测试了这些化合物对革兰氏 +的生物学活性。 和Gram -细菌。在这些化合物中,(E)-1-(4-氯苄基)-5-styrylindoline-2、3-二酮对大肠杆菌表现出良好的抗菌活性(Gram -),对金黄色葡萄球菌具有中等的抗菌活性。 (Gram + )。

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