Neto Íris, Andrade Joana, Fernandes A S, Pinto Reis Catarina, Salunke Jagadish K, Priimagi Arri, Candeias Nuno R, Rijo Patrícia
Center for Research in Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, 1749-024, Lisboa, Portugal.
Department of Chemistry and Bioengineering, Tampere University of Technology, Korkeakoulunkatu 8, 33101, Tampere, Finland.
ChemMedChem. 2016 Sep 20;11(18):2015-23. doi: 10.1002/cmdc.201600244. Epub 2016 Jul 26.
In this work we report the antibacterial activity of alkylaminophenols. A series of such compounds was prepared by a multicomponent Petasis-borono Mannich reaction starting from salicylaldehyde and its derivatives. The obtained compounds were tested against a large panel of microorganisms, Gram-positive and Gram-negative bacteria, and a yeast. Among the several tertiary amine derivatives tested, indoline-derived aminophenols containing a nitro group at the para-phenol position showed considerable activity against bacteria tested with minimal inhibitory concentrations as low as 1.36 μm against Staphyloccocus aureus and Mycobacterium smegmatis. Cytotoxicity of the new para-nitrophenol derivatives was observed only at concentrations much higher than those required for antibacterial activity.
在本研究中，我们报道了烷基氨基酚的抗菌活性。通过多组分Petasis-硼诺曼尼希反应，以水杨醛及其衍生物为起始原料，制备了一系列此类化合物。所得到的化合物针对大量微生物进行了测试，包括革兰氏阳性菌、革兰氏阴性菌以及一种酵母。在测试的几种叔胺衍生物中，在对苯酚对位含有硝基的吲哚啉衍生氨基酚对所测试的细菌表现出相当的活性，对金黄色葡萄球菌和耻垢分枝杆菌的最低抑菌浓度低至1.36 μm。仅在远高于抗菌活性所需浓度时才观察到新型对硝基苯酚衍生物的细胞毒性。
