|
|||||
|
|
| 有机磷酸酯解毒剂嘧啶甲醛肟季铵盐及其衍生物的合成 | |
| 引用本文： | 禹茂章,朱淬砺. 有机磷酸酯解毒剂嘧啶甲醛肟季铵盐及其衍生物的合成[J]. 药学学报, 1982, 17(8): 624-628 |
| 作者姓名： | 禹茂章 朱淬砺 |
| 作者单位： | 上海第一医学院药学系合成药物化学教研室，上海第一医学院药学系合成药物化学教研室 化工部科学技术情报研究所 |
| 摘 要： | 解磷定(I,2-PAM)对有机磷农药中毒的解毒机理,系由其分子中的肟基阴离子向中毒的磷酰化乙酰胆碱酯酶(AcChE)的磷原子作亲核进攻,致使磷酰基断裂而使AcChE复能。因此,醛肟基的pKa可能与AcChE的复能活性之间存在一定联系。Childs曾报道嘧啶-2-异羟肟酸(Ⅱ)和Ashani等报道4-嘧啶甲醛肟碘甲烷季铵盐(Ⅲ_b),分别对沙林(sarin)和异氟磷(DFP)有一定复能作用。为此,作者合成了一些不同位置的嘧啶甲醛 |
| 关 键 词： | 乙酰胆碱酯酶复能剂 亚硝化反应 嘧啶甲醛肟 嘧啶甲醛肟碘(氯)甲烷季铵盐 |
| 收稿时间： | 1981-10-13 |
SYNTHESIS OF QUATERNARY SALTS OF HYDROXIMINOMETHYLPYRIMIDINES AND THEIR DERIVATIVES AS ANTIDOTES AGAINST ORGANOPHOSPHATE POISONING |
|
| YU Mao-zhang and ZHU Cui-li. SYNTHESIS OF QUATERNARY SALTS OF HYDROXIMINOMETHYLPYRIMIDINES AND THEIR DERIVATIVES AS ANTIDOTES AGAINST ORGANOPHOSPHATE POISONING[J]. Acta pharmaceutica Sinica, 1982, 17(8): 624-628 | |
| Authors: | YU Mao-zhang and ZHU Cui-li |
| Abstract: | Five quaternary salts of hydroximinomethyl-pyrimidines and their derivatives (Ⅲa～Ⅲc) were synthesized, and their reactivation activities for phosphorylated acetylcholinesterase were studied. These compounds were prepared by quaternization of corresponding hydroximinomethyl-pyrimidines obtained from nitrosation of methyl-pyrimidines with isoamyl nitrite in absolute alcohol in the presence of hydrogen chloride, or by nitrosation of quaternary salts of methylpyrimidines under similar Conditions.Preliminary pharmacological examination showed that these compounds, except Ⅲc have no effect in the protection against Paraoxon (E600) intoxication in mice.However, for the reactivation of Paraoxon inhibited acetylcholinesterase Ⅲa～Ⅲc, are as effective as 2-PAM in vitro. |
| Keywords: | Reactivator of inhibited AcChE Nitrosation Hydroximinomethylpyrimidines Hydroximinomethyl-pyrimidinium methiodides (methyl chlorides) |
| 本文献已被 CNKI 等数据库收录！ | |
| 点击此处可从《药学学报》浏览原始摘要信息 | |
| 点击此处可从《药学学报》下载全文 | |