噻二唑基-3-哒嗪酮类化合物的合成及生物活性

Synthesis and Biological Activities of New Thiadiazolyl 3-pyridazinones

摘要: 将取代的二酰基肼环合后,得到中间体2-芳基-5-氯甲基-1,3,4-噻二唑,然后与2-叔丁基-4-氯-5-羟基-3(2H)-哒嗪酮反应,合成了8个未见文献报道的含噻二唑基哒嗪酮类化合物,其化学结构经1H NMR、高分辩质谱和元素分析确认。生物活性测试结果表明,部分化合物对粘虫P.separate W.有较好的抑制生长活性,其中化合物 3b 的EC50值为21 mg/L。

Abstract: Eight new thiadiazolyl 3(2H)-pyridazinones compounds were synthesized by the reaction of 2-tert-butyl-4-chloro-5-hydroxy-3(2H)-pyridazinones with 5-aryl-2-chloromethyl-1,3,4-oxadiazoles which were prepared by the cyclization of N-chloroacetyl-N'-aroylhydrazines. The structure of the title compounds were confirmed by 1H NMR, HR mass spectra and elemental analysis. Their biological activities were examined and some of them exhibited good activities against Pseudaletia separate Walker. The EC50 of 3b was 21 mg/L.