Synthesis and Structure-Activity Relationship of Palmatine Derivatives as a Novel Class of Antibacterial Agents against Helicobacter pylori
文献类型:期刊论文
作者 | Fan, Tianyun1; Guo, Xixi1; Zeng, Qingxuan1; Wei, Wei1; You, Xuefu1; Pang, Jing1; Wang, Yanxiang1,2; Song, Danqing1 |
刊名 | MOLECULES |
出版日期 | 2020-03-02 |
卷号 | 25期号:6页码:12 |
关键词 | Helicobacter pylori palmatine synthesis structure-activity relationship urease |
DOI | 10.3390/molecules25061352 |
通讯作者 | Pang, Jing(pangjing.pangjing@163.com) ; Wang, Yanxiang(wangyanxiang@imb.pumc.edu.cn) |
英文摘要 | Taking palmatine (PMT) as the lead, 20 new PMT derivatives were synthesized and examined for their antibacterial activities against six tested metronidazole (MTZ)-resistant Helicobacter pylori (H. pylori) strains. The structure-activity relationship (SAR) indicated that the introduction of a suitable secondary amine substituent at the 9-position might be beneficial for potency. Among them, compound 1c exhibited the most potent activities against MTZ-resistant strains, with minimum inhibitory concentration (MIC) values of 4-16 mu g/mL, better than that of the lead. It also exhibited a good safety profile with a half-lethal dose (LD50) of over 1000 mg/kg. Meanwhile, 1c might exert its antimicrobial activity through targeting H. pylori urease. These results suggested that PMT derivatives might be a new family of anti-H. pylori components. |
WOS关键词 | ANTIMICROBIAL ACTIVITY ; UREASE ; ACID |
资助项目 | CAMS initiative for innovative medicine[2019-I2M-1-005] ; CAMS initiative for innovative medicine[2017-I2M-1-012] ; CAMS initiative for innovative medicine[2016-I2M-1-011] ; National Natural Science Foundation of China[81603195] |
WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
语种 | 英语 |
出版者 | MDPI |
WOS记录号 | WOS:000530248700095 |
源URL | [http://119.78.100.183/handle/2S10ELR8/280288] |
专题 | 中国科学院上海药物研究所 |
通讯作者 | Pang, Jing; Wang, Yanxiang |
作者单位 | 1.Chinese Acad Med Sci & Peking Union Med Coll, Beijing Key Lab Antimicrobial Agents, Inst Med Biotechnol, Beijing 100050, Peoples R China 2.Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Medica, State Key Lab Bioact Substance & Funct Nat Med, Beijing 100050, Peoples R China |
推荐引用方式 GB/T 7714 | Fan, Tianyun,Guo, Xixi,Zeng, Qingxuan,et al. Synthesis and Structure-Activity Relationship of Palmatine Derivatives as a Novel Class of Antibacterial Agents against Helicobacter pylori[J]. MOLECULES,2020,25(6):12. |
APA | Fan, Tianyun.,Guo, Xixi.,Zeng, Qingxuan.,Wei, Wei.,You, Xuefu.,...&Song, Danqing.(2020).Synthesis and Structure-Activity Relationship of Palmatine Derivatives as a Novel Class of Antibacterial Agents against Helicobacter pylori.MOLECULES,25(6),12. |
MLA | Fan, Tianyun,et al."Synthesis and Structure-Activity Relationship of Palmatine Derivatives as a Novel Class of Antibacterial Agents against Helicobacter pylori".MOLECULES 25.6(2020):12. |
入库方式: OAI收割
来源:上海药物研究所
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