| 論文名 |
Functionalized cyclodextrins bearing an alpha nucleophile--a promising way to degrade nerve agents. |
| 著者 |
Estour F
Letort S
M?ller S
Kalakuntla RK
Le Provost R
Wille T
Reiter G
Worek F
Lafont O
Gouhier G
|
| キーワード |
|
| 出版年月 |
1970年1月 |
| 発表先 |
Chem Biol Interact. 2013 Mar 25;203(1):202-7. |
| WEBサイト |
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| 論文概要（和文） |
アルファ求核剤を有する機能化されたシクロデキストリン-神経物質を分解する有望な方法。 |
| 論文概要（英文） |
Organophosphorus nerve agents are irreversible inhibitors of acetylcholinesterase. Current treatment of nerve agent poisoning has limited efficacy and more efficient medical countermeasures need to be developed. A promising approach is to design chemical scavengers more stable during storage and less immunogenic than bioscavengers. Furthermore, they could be produced at lowest production costs. Cyclodextrins are attractive cyclic oligosaccharides that can be used to develop chemical scavengers of organophosphorus nerve agents. Their abilities to form inclusion and non-inclusion complexes with organic substrates are useful to trap chemical warfare agents. Selective introduction of an α-nucleophile residue on the secondary face of β-cyclodextrin allowed to obtain supramolecular derivatives active against organophosphorus compounds. The degradation activity of these monosubstituted cyclodextrins was determined against paraoxon and chemical warfare agents. These tests showed that the structure of the scavengers mainly influences the interaction between the organophosphorus substrate, or its reaction products, and the cyclodextrin moiety. All the tested G-type agents were efficiently degraded. According to the binding modes of cyclosarin, some oligosaccharidic scavengers led to an enantioselective degradation of this nerve agent. These promising derivatives open the way to further investigations of new structural modifications to reach more sophisticated and efficient scavengers for prophylactic and curative medical applications. |
