derivativesofaryl4guanidinomethylbenzoateandnaryl4guanidinomethylbenzamideasnewantibacterialagentssynthesisandbioactivity
文献类型：期刊论文
| 作者 | Wenyuan YU1; Lixia YANG1; Jianshu XIE2; Ling ZHOU1; Xueyuan JIANG3; Dexu ZHU3; Mutsumi MURAMATSU3; Mingwei WANG1
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| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2008 |
| 卷号 | 29期号:2页码:267 |
| 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 |
| ISSN号 | 1671-4083 |
| 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： Atotal of 44 derivatives of aryl-4-guanidin- omethylbenzoate （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 μg/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. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/285840]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国科学院上海药物研究所 2.Shanghai East Best Biopharmaceutical Enterprises Co Ltd 3.南京大学 |
| 推荐引用方式 GB/T 7714 | Wenyuan YU,Lixia YANG,Jianshu XIE,et al. derivativesofaryl4guanidinomethylbenzoateandnaryl4guanidinomethylbenzamideasnewantibacterialagentssynthesisandbioactivity[J]. actapharmacologicasinica,2008,29(2):267. |
| APA | Wenyuan YU.,Lixia YANG.,Jianshu XIE.,Ling ZHOU.,Xueyuan JIANG.,...&Mingwei WANG.(2008).derivativesofaryl4guanidinomethylbenzoateandnaryl4guanidinomethylbenzamideasnewantibacterialagentssynthesisandbioactivity.actapharmacologicasinica,29(2),267. |
| MLA | Wenyuan YU,et al."derivativesofaryl4guanidinomethylbenzoateandnaryl4guanidinomethylbenzamideasnewantibacterialagentssynthesisandbioactivity".actapharmacologicasinica 29.2(2008):267. |
入库方式： OAI收割
来源：上海药物研究所
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