李周华,杨雅聪,陈雪冬,等.2-氨基吩噁嗪-3-酮类化合物的合成及其生物活性评价[J].中国海洋药物,2021,40(6):30-36.
2-氨基吩噁嗪-3-酮类化合物的合成及其生物活性评价
Synthesis and Evaluation of the bioactivity of 2- aminophenoxazine -3- ketones from Halomonas
投稿时间:2021-01-20  修订日期:2021-03-08
DOI:
中文关键词:  次级代谢产物  抗菌活性  耐药菌
English Keywords:secondary metabolite  antibacterial activity  drug-resistance bacteria
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作者单位E-mail
李周华 中国海洋大学 lizhouhua960808@163.com 
杨雅聪 中国海洋大学医药学院  
陈雪冬 中国海洋大学医药学院  
徐锡明 中国海洋大学医药学院  
王一帆 中国海洋大学食品科学与工程学院  
柳晓春 中国海洋大学医药学院  
唐宇 中国海洋大学医药学院 tangyu@ouc.edu.cn 
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中文摘要:
      目的 2-氨基吩噁嗪-3-酮类化合物的合成及其生物活性评价。方法 以苄基保护甲基香兰素为初始原料经过格氏反应、Oppenauer氧化、氧化环合等反应,7步合成8-苯甲酰基-2-氨基-6-羟基-吩噁嗪-3-酮类化合物,并对其进行抗菌、抗癌等活性的测试。 结果 合成了天然产物8-苯甲酰基-2-氨基-6-羟基-吩噁嗪-3-酮,通过对其进行抗菌活性测试,发现其对耐甲氧西林凝固酶阴性葡萄球菌和耐甲氧西林金黄色葡萄球菌的抑制作用均优于环丙沙星,最小抑菌浓度(MIC)分别为0.390 μM,6.250 μM。通过酶水平活性测试,发现此天然产物对TBK1(TANK-binding kinase 1 )的抑制活性与阳性对照药氨来占诺相近。
English Summary:
      Objective To study the structure and biological activity of 2-amino-8-benzoyl-6-hydroxy-3H-phenoxazin-3-one from Halomonas. Methods 2-amino-8-benzoyl-6-hydroxy-3H-phenoxazin-3-one was synthesized from benzyl protective methyl vanillin in 7 steps by grigner reagent, Oppenauer oxidation and oxidation cyclization, and its antibacterial and anticancer activities were tested. Results The natural product 2-amino-8-benzoyl-6-hydroxy-3H-phenoxazin-3-one was synthesized, and the bioactivity test showed that its inhibitory effect on MRCNS (0.390 μM) and MRSA (6.250 μM) of methicillin-resistant Staphylococcus aureus was superior to that of ciprofloxacin. After molecular docking and enzyme activity tests, the inhibition of the natural product on TBK1 activity was similar to that of the positive control drug Aminoxanol.
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