論文 - 詳細
| RRC ID | 61271 |
|---|---|
| 著者 | Ohkura K, Sukeno A, Nagamune H, Kourai H. |
| タイトル | Bridge-linked bis-quaternary ammonium anti-microbial agents: relationship between cytotoxicity and anti-bacterial activity of 5,5'-[2,2'-(tetramethylenedicarbonyldioxy)-diethyl]bis(3-alkyl-4-methylthiazonium iodide)s. |
| ジャーナル | Bioorg Med Chem |
| Abstract |
We examined the correlation between the anti-bacterial activity against Escherichia coli and the cytotoxicity of five synthesized bridge types of bis-quaternary ammonium compounds (bis-QACs) as follows: thioether type, 4,4'-(p-xylydithio)bis(1-octylpyridinium iodide) (4DTBP-X,8); amide type, N,N'-tetramethylenebis(1-dodecyl-4-carbamoylpyridinium iodide) (4BCAP-4,12), N,N'-(phenylene)bis(1-octyl-4-carbamoylpyridinium iodide) (4BCAP-P,8); anti-amide type, 4,4'-(tetramethylenedicarbonyldiamino)bis(1-octylpyridinium iodide) (4DCABP-4,8), 4,4'-(phenylenedicarbonyldiamino)bis(1-octylpyridinium iodide) (4DCABP-P,8); ester type, 4,4'-(1,6-hexamethylenedioxydicarbonyl)bis(1-dodecylpyridinium iodide) (4DOCBP-6,12); and an anti-ester type, 5,5'-[2,2'-(tetramethylenedicarbonyldioxy)diethyl]bis(3-alkyl-4-methylthiazolium iodide) (5DEBT-4,n, The letter n indicates the carbon number of the alkyl group). 5DEBT-4,8 showed low cytotoxicity (LD(50)) to human erythrocytes (97+/-6microM) and the NB1RGB cell line (111+/-20microM) and remarkable anti-bacterial activity (MIC) toward E. coli K12 W3110 (7.9microM). Moreover, 5DEBT-4,8 indicated 1144 conformers by global minimum analysis and had two minimum dGW (solvation free energy) points as well as 4DTBP-6,8, which had been previously examined and concluded to be a significant useful anti-bacterial compound. |
| 巻・号 | 13(7) |
| ページ | 2579-87 |
| 公開日 | 2005-4-1 |
| DOI | 10.1016/j.bmc.2005.01.030 |
| PII | S0968-0896(05)00055-6 |
| PMID | 15755659 |
| MeSH | Anti-Bacterial Agents / chemistry Anti-Bacterial Agents / pharmacology* Cell Line Cell Survival / drug effects Erythrocytes / drug effects Escherichia coli / drug effects Fibroblasts / drug effects Humans Microbial Sensitivity Tests Models, Molecular Molecular Structure Quaternary Ammonium Compounds / chemistry* Quaternary Ammonium Compounds / pharmacology* Structure-Activity Relationship |
| IF | 3.073 |
| オルトメトリクス指標 |
オルトメトリクス指標項目
|
| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 4 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | NB1RGB(RCB0222) |