Synthesis, characterization and biological evaluation of some newer carbazole derivatives
作者:Divyanshu Sharma、Nitin Kumar、Devender Pathak
DOI:10.2298/jsc130123069s
日期:——
5-((9H-carbazol-9-yl)methyl)-N-((substituted phenyl)(piperazin-1-yl)methyl)-1,3,4-oxadiazol-2-amine (4a-4o) derivatives was synthesized by starting with carbazole which on reaction with ethyl choloroacetate yielded ethyl 2-(9H-carbazole-9-yl)acetate (1), compound (1) on reaction with semicarbazide followed by cyclisation with sulphuric acid gave 5-((9H-carbazole-9-yl)-1,3,4-oxadiazol-2-amine (3) which through Mannich
一系列新颖的5-((9H-咔唑-9-基)甲基)-N-((取代的苯基)(哌嗪-1-基)甲基)-1,3,4-恶二唑-2-胺(4a-通过咔唑开始合成4o)衍生物,咔唑与氯代乙酸乙酯反应生成2-(9H-咔唑-9-基)乙酸乙酯(1),化合物(1)与氨基脲反应,然后用硫酸环化得到5- ((9H-咔唑-9-基)-1,3,4-恶二唑-2-胺(3)在乙酸的存在下通过与哌嗪和各种芳族醛的曼尼希反应生成标题化合物(4a- 4o)。通过紫外,傅立叶红外光谱,1H-NMR,MS光谱研究和元素分析对化合物的结构进行了表征,评估了所有衍生物的抗菌,抗真菌和抗癌活性,其中所测试的化合物4a,4d,4e和4n显示出显着的抗菌和抗真菌活性,而发现化合物4a,4d,4k和4n对人乳腺癌细胞系即MCF7具有活性。