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Novel reactivators against tabun- and paraoxon-inhibited acetylcholinesterase

등록일
2007년 8월 10일 16시 15분 03초
접수번호
0282
발표코드
35P278포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 <발표Ⅱ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
Kamil Musilek, Daniel Jun, 정영식1, Kamil Kuca
Faculty of Military Health Sciences, Czech Republic,
1한국화학연구원 신약연구단,

The reactivators of acetylcholinesterase (AChE, EC 3.1.1.7) are very important components in the treatment of intoxications caused by organophosphate inhibitors such as nerve agents and pesticides. These inhibitors covalently bind to active site of mentioned enzyme and irreversibly inhibit its activity. The reactivator breaks the inhibitor-enzyme covalent bond and restores its activity. Unfortunately, there is no reactivator applicable for every type of inhibitor; it means that every structural change in the molecule of inhibitor needs a specific structure of the reactivator. More than 100 compounds was prepared and evaluated in our department since 2004. Some reactivators were able to exceed potency of commercial available compounds in vitro. The SAR study was used to select more active reactivators. The key features of the reactivator’s molecule were determined.

The work was supported by the Grant Agency of Ministry of Education, Youth and Sports (Czech Republic) – grant no. ME865.


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