Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity
文献类型：期刊论文
| 作者 | Yu, Wen-yuan2; Yang, Li-xia2; Xie, Jian-shu3; Zhou, Ling2; Jiang, Xue-yuan1; Zhu, De-xu1; Muramatsu, Mutsumi1; Wang, Ming-wei2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2008-02 |
| 卷号 | 29期号:2页码:267-277 |
| 关键词 | antibacterial agents drug-resistant bacteria Gram-positive bacteria |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2008.00720.x |
| 文献子类 | Article |
| 英文摘要 | Aim: The aim of the present study was to design, synthesize, and evaluate novel antibacterial agents, derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide. Methods: A total of 44 derivatives of aryl-4-guanidinomethylbenzoate (series A) and N-aryl-4-guanidinomethylbenzamide (series B) were synthesized and their antibacterial activities were assessed in vitro against a variety of Gram-positive and Gram-negative bacteria by an agar dilution method. Results: Twelve compounds showed potent bactericidal effects against a panel of Gram-positive germs, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), vancomycin-intermediate Staphylococcus aureus (VISA), and methicillin-resistant coagulase-negative staphylococci (MRCNS), with minimum inhibitory concentrations (MIC) ranging between 0.5 and 8 mu g/mL, which were comparable to the MIC values of several marketed antibiotics. They exhibited weak or no activity on the Gram-negative bacteria tested. In addition, these compounds displayed high inhibitory activities towards oligopeptidase B of bacterial origin. Conclusion: In comparison with the previously reported MIC values of several known antibiotics, the derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide showed comparable in vitro bactericidal activities against VRE and VISA as linezolid. Their growth inhibitory effects on MRSA were similar to vancomycin, but were less potent than linezolid and vancomycin against MRCNS. This class of compounds may have the potential to be developed into narrow spectrum antibacterial agents against certain drug-resistant strains of bacteria. |
| WOS关键词 | NATURAL GUANIDINE DERIVATIVES ; RESISTANT STAPHYLOCOCCUS-AUREUS ; ACID 4-TERT-BUTYLPHENYL ESTER ; ESCHERICHIA-COLI ; OLIGOPEPTIDASE-B ; IN-VITRO ; ENTEROCOCCUS-FAECIUM ; HELICOBACTER-PYLORI ; TRYPSIN-INHIBITOR ; SIGNAL PEPTIDE |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3249771 |
| WOS记录号 | WOS:000252805200019 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272983]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Wang, Ming-wei |
| 作者单位 | 1.Nanjing Univ, Dept Biochem, Nanjing 210093, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 3.Shanghai E Best Biopharmaceut Enterprises Co Ltd, Shanghai 200233, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yu, Wen-yuan,Yang, Li-xia,Xie, Jian-shu,et al. Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity[J]. ACTA PHARMACOLOGICA SINICA,2008,29(2):267-277. |
| APA | Yu, Wen-yuan.,Yang, Li-xia.,Xie, Jian-shu.,Zhou, Ling.,Jiang, Xue-yuan.,...&Wang, Ming-wei.(2008).Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity.ACTA PHARMACOLOGICA SINICA,29(2),267-277. |
| MLA | Yu, Wen-yuan,et al."Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity".ACTA PHARMACOLOGICA SINICA 29.2(2008):267-277. |
入库方式： OAI收割
来源：上海药物研究所
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