喹啉酮类化合物抗幽门螺杆菌的构效关系研究
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摘要
用体外平板打孔法对4-喹啉酮类化合物进行抗幽门螺杆菌活性试验,探究了4-喹啉酮类化合物抗幽门螺杆菌活性的构效关系。结果表明:2-己基-3-甲基喹啉酮抗幽门螺杆菌效果最好,4-喹啉酮N-1位取代使抗幽门螺杆菌活性下降或消失; C-2位取代为己烷基,活性最佳;C-3位取代可使活性增加,C-3位甲基取代为必要结构可使活性显著增加; C-6位及C-7位取代使活性降低。
Objective: To explore the structure-activity relationship of 4-quinolinones against Helicobacter pylori. Methods: Incubating plate with foveolae was used to study the Anti-helicobacter pylori activity of 4-quinolinones. Results: 2-hexyl-3-methyl Quinolinone has the best effect against helicobacter pylori. Conclusion: The activity of anti-helicobactor pylori will decrease with the substitution for N-1,C-6,C-7 positionof 4-quinolinones. The activity is the best when the substitution for C-2 position is hexyl. The activity will increase with the substitution for C-3 position,especially methyl.
Objective: To explore the structure-activity relationship of 4-quinolinones against Helicobacter pylori. Methods: Incubating plate with foveolae was used to study the Anti-helicobacter pylori activity of 4-quinolinones. Results: 2-hexyl-3-methyl Quinolinone has the best effect against helicobacter pylori. Conclusion: The activity of anti-helicobactor pylori will decrease with the substitution for N-1,C-6,C-7 positionof 4-quinolinones. The activity is the best when the substitution for C-2 position is hexyl. The activity will increase with the substitution for C-3 position,especially methyl.
引文
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[8] DEKKER K A,INAGAKI T,GOOTZ T D,et al. New quinolone compounds from Pseudonocardia sp. with selective and potent anti-Helicobacter pylori activity:taxonomy of producing strain,fermentation,isolation,structural elucidation and biological activities[J]. Journal of Antibiotics,2010,29(27):112-114.
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[11]钟猛,丁锐,林华鑫,等.吡啶衍生物合成及抗幽门螺杆菌活性研究[J].重庆理工大学学报(自然科学),2017,31(5):105-110.
[12] RHO T C,BAE E A,KIM D H,et al. Anti-Helicobacter pylori activity of quinolone alkaloids from Evodiae fructus[J]. Biological&Pharmaceutical Bulletin,1999,22(10):1141-1143.
[2]谢润勇.雷贝拉唑三联疗法治疗幽门螺杆菌相关性消化性溃疡的临床研究[J].中国当代医药,2013,20(1):91-92.
[3]刘东振.幽门螺杆菌相关性疾病及根除治疗现状与进展[J].医学理论与实践,2013(22):2969-2971.
[4]甘远,黄方华,王瑞云,等.幽门螺杆菌感染的治疗现状及进展[J].海南医学,2016,27(9):1483-1485.
[5]李明.幽门螺杆菌感染的治疗现状[J].齐齐哈尔医学院学报,2013,34(6):864-865.
[6] TOHRU S. Limonoids and quinolone alkaloids from Evodia rutaecarpa Benthan[J]. Chem Pharm Bul I,1988,56(1I):5.
[7] HAMASAKI N,ISHII E,TOMINAGA K,et al. Highly Selective Antibacterial Activity of Novel Alkyl Quinolone Alkaloids from a Chinese Herbal Medicine,Gosyuyu(Wu-Chu-Yu),against[J]. Microbiology&Immunology,2008,44(1):9-15.
[8] DEKKER K A,INAGAKI T,GOOTZ T D,et al. New quinolone compounds from Pseudonocardia sp. with selective and potent anti-Helicobacter pylori activity:taxonomy of producing strain,fermentation,isolation,structural elucidation and biological activities[J]. Journal of Antibiotics,2010,29(27):112-114.
[9] MURI E M,WILLIAMSON J S. Anti-Helicobacter pylori agents. An update[J]. Mini Reviews in Medicinal Chemistry,2004,4(2):69-74.
[10] SHAHID S K. Novel anti-Helicobacter pylori therapies[J]. Pharmaceutical patent analyst,2014,3(4):411-427.
[11]钟猛,丁锐,林华鑫,等.吡啶衍生物合成及抗幽门螺杆菌活性研究[J].重庆理工大学学报(自然科学),2017,31(5):105-110.
[12] RHO T C,BAE E A,KIM D H,et al. Anti-Helicobacter pylori activity of quinolone alkaloids from Evodiae fructus[J]. Biological&Pharmaceutical Bulletin,1999,22(10):1141-1143.