新型双花素基腙和肟的合成、抗菌及细胞毒性活性
Synthesis, antibacterial and cytotoxic activities of new biflorin-based hydrazones and oximes.
作者信息
da S Souza Luciana G, Almeida Macia C S, Lemos Telma L G, Ribeiro Paulo R V, de Brito Edy S, Silva Vera L M, Silva Artur M S, Braz-Filho Raimundo, Costa José G M, Rodrigues Fábio F G, Barreto Francisco S, de Moraes Manoel O
机构信息
Departamento de Química Orgânica e Inorgânica, Universidade Federal do Ceará, Campus do Pici, 60451-970 Fortaleza, CE, Brazil.
Departamento de Química Orgânica e Inorgânica, Universidade Federal do Ceará, Campus do Pici, 60451-970 Fortaleza, CE, Brazil.
出版信息
Bioorg Med Chem Lett. 2016 Jan 15;26(2):435-439. doi: 10.1016/j.bmcl.2015.11.095. Epub 2015 Nov 27.
Biflorin 1 is a biologically active quinone, isolated from Capraria biflora. Five new biflorin-based nitrogen derivatives were synthesized, of which two were mixtures of (E)- and (Z)- isomers: (Z)-2a, (Z)-2b, (Z)-3a, (Z)- and (E)-3b, (Z)- and (E)-3c. The antibacterial activity was investigated using the microdilution method for determining the minimum inhibitory concentration (MIC) against six bacterial strains. Tests have shown that these derivatives have potential against all bacterial strains. The cytotoxic activity was also evaluated against three strains of cancer cells, but none of the derivatives showed activity.
双花醌1是一种从双花藿香蓟中分离出的具有生物活性的醌类化合物。合成了五种基于双花醌的新型含氮衍生物，其中两种是（E）-和（Z）-异构体的混合物：（Z）-2a、（Z）-2b、（Z）-3a、（Z）-和（E）-3b、（Z）-和（E）-3c。采用微量稀释法研究了这些衍生物对六种细菌菌株的抗菌活性，以确定最低抑菌浓度（MIC）。测试表明，这些衍生物对所有细菌菌株都有潜在活性。还评估了这些衍生物对三种癌细胞株的细胞毒性活性，但没有一种衍生物显示出活性。
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