根据生物等排原理和新烟碱类化合物与乙酰胆碱酯酶的作用机理,以4-噻唑啉酮(4)为中间体设计合成了2-取代-3-(2-氯-5-吡啶亚甲基)-4-氰基亚胺基-1,3-噻唑烷(Sa~8c)和5-芳基次甲基-2-芳基-3-(2-氯-5-吡啶亚甲基)4-噻唑啉酮(Sa~5e)两类化合物。中间体(4)由醛、胺和巯基乙酸缩合得到。所有化合物的结构均经元素分析和^1H NMR确证。初步生物活性试验结果表明,部分化合物具有一定的杀菌活性和促进黄瓜子叶生根活性,化合物8b显示出很好的抗HIV-1蛋白酶活性。
According to bioisosteric relationship and the mode of action between Neonicotinoid compounds and acetylcholin esterase, two series of Neonicotinoid compounds 2-substituted-3-(2-chloro-5-pyridinemethylene)- 4-cyanoimino-1,3-thiazolidine ( 8a--8c ) and 5-arylidene-2-aryl-3-( 2-chloro-5-pyridinemethylene ) -4-thiazo- lidinones(Sa--5e) were designed and synthesized from 4-thiazolidinones (4). Intermediates 4 were synthe- sized by the condensation of amine, aldehyde and mercapto acetic acid. Their structures were character-ized via elemental analysis, ^1H NMR spectra. The preliminary bioassay results show that some title compounds exhibited certain fungicidal activities, promoting cucumber cotyledon root-formation activities and compound 8b showed favourable anti-HIV PR.