Chemical reactivity and antimicrobial activity of <i>N</i>-substituted maleimides
作者:Natalia Salewska、Joanna Boros-Majewska、Izabela Łącka、Katarzyna Chylińska、Michał Sabisz、Sławomir Milewski、Maria J. Milewska
DOI:10.3109/14756366.2011.580455
日期:2012.2.1
µg ml(-1). Low antimicrobial but high cytostatic activity was noted for basic maleimides containing tertiary aminoalkyl substituents. Chemical reactivity and lipophilicity influenced antibacterial activity of neutral maleimides but had little if any effect on their antifungal and cytostatic action. N-substituted maleimides affected biosynthesis of chitin and β(1,3)glucan, components of the fungal cell
合成了几种含有具有变化的体积和极性的取代基的N-取代的马来酰亚胺,并测试了其抗微生物和细胞抑制活性。中性马来酰亚胺显示相对较强的抗真菌作用的最小抑制浓度(MIC在0.5-4 µg ml(-1)范围内);它们的抗菌活性是结构依赖性的,并且都具有高度的细胞抑制作用,IC(50)值低于0.1 µg ml(-1)。对于含有叔氨基烷基取代基的碱性马来酰亚胺,抗菌性低,但具有较高的细胞抑制活性。化学反应性和亲脂性影响中性马来酰亚胺的抗菌活性,但对其抗真菌和细胞抑制作用几乎没有影响。N-取代的马来酰亚胺影响几丁质和β(1,3)葡聚糖,真菌细胞壁的组成部分的生物合成。膜酶β(1