以(取代)水杨醛、间(对)羧基苯胺和氨基甲酰肼为原料,分别采用冰浴法合成了4-(二乙基氨基)水杨醛-3-羧基苯胺(3a),4-(二乙基氨基)水杨醛-4-羧基苯胺(3b)和水杨醛-3-羧基苯胺(3c);采用固相法合成了4-(二乙基氨基)水杨醛-氨基甲酰肼(3d);采用水浴回流法合成了3,5-二溴水杨醛-4-羧基苯胺(3e)和2-羟基-1-萘甲醛-4-羧基苯胺(3f),3a~3f均为新化合物,其结构经1H NMR,IR,ESI-MS和元素分析表征。研究了3a~3f对大肠杆菌、金黄色葡萄球菌及欧文氏草生杆菌的抑菌活性。结果表明:3a~3f对受试菌种均有一定的抑菌活性,其中3e的抑菌活性最好。
Using( substituted) salicylaldehyde,m( p)-carboxyaniline and carbamoyl hydrazine as the raw materials,4-( diethylamino) salicylaldehyde-3-carboxyaniline( 3a),4-( diethylamino) salicylaldehyde-4-carboxy aniline( 3b) and salicylaldehyde-3-carboxy-aniline( 3c) were synthesized by the ice bath method,4-( diethylamino) salicylaldehyde-amino acid hydrazide( 3d) was synthesized by the solid-phase method,3,5-dibromo salicylaldehyde-4-carboxyaniline( 3e) and 2-hydroxy-1-naphthaldehyde-4-carboxyaniline( 3f) were synthesized by the reflux method. 3a ~ 3f were novel compounds.The structures were characterized by1 H NMR,IR,ESI-MS and elemental analysis. The antimicrobial activities of 3a ~ 3f against S. aureus,E. herbicola and E. coli were investigated. The results showed that 3a ~ 3f exhibited certain biological activities,and 3e was the best one.