《3-取代硫基-4-N-邻羟苯基亚胺基-5-乙基-1,2,4-三唑类化合物的合成及抑菌活性》.pdf.pdf

第27卷第5-6期 2011年12月天津工大学学报 JoURNAL oF TIANJIN UNIVERSITY oF TECHNoLoGY 文章编号:1673—095X(2011)05—06—0008—05 3-取代硫基-4一N一邻羟苯基亚***基一5一乙基-1,2, 4一三唑类化合物的合成及抑菌活性穆曼曼1,卢俊瑞1,辛春伟1,卢博为2,戢丹1,鲍秀荣1 (,天津300384;,天津300071) 摘要:本文以对称二氨基硫脲为原料,经关环,缩合,亲核取代反应,合成出5个新型抗菌剂一3一取代硫基一4一N一邻羟苯基亚***,2,4一三唑类化合物(3a~3e),并利用1HNMR,, %时,%;对大肠杆菌的抑茵率高于 80%.构效关系表明,三唑硫醚类化合物对革兰氏阳性茵(金黄色葡萄球菌)的抑制效果强于三唑硫醇类化合物;苯乙酰***环的对位上引入拉电子基团如一Cl,一Br,一NO,可增加化合物的抑茵活性,而引入推电子基团如一CH,则降低其抑茵活性;与现售药物***康唑相比,所合成的目标化合物的抗茵效果更优. 关键词:3一取代硫基-4一N一邻羟苯基亚***基-,2,4一三唑;合成;抑菌活性中图分类号: 文献标识码:A doi:.1673-- Synthesis and antibacterial activities of3--substituted sulfur--4·-N·- (2-hydroxyphenyl)imino-5-ethyl-1,2,4-triazole MU ,LU Jun—ruil,XIN ,LU ,JI Danl,BAO ( ofChemistry and Chemical En百neefing,Tianjin University ofTechnology,Tianjin 300384,China; ofChemistry,Nankai University,Tianjin300071,China) Abstract:Five novel antibacterial agent一3一substituted sulfur-4一N一(2一hydroxyphenyl)imino一5-ethyl-1,2,4一triazole (3a~3e)were designed and synthesized bycyclization,condensation and nucleophilic substitution structures pounds were characterized by IRand resultsofpreliminary bioassay showed pounds 3a一3e have more than90%inhibitory rate against us aureus and Mo