Salmi Chanaz, Loncle Celine, Vidal Nicolas, Laget Michéle, Letourneux Yves, Brunel Jean Michel
Laboratoire SESNAB, UMR-MD1, case 342, Faculté de St Jérome, Université de Méditerranée, Marseille, Cedex 20, France.
J Enzyme Inhib Med Chem. 2008 Dec;23(6):860-5. doi: 10.1080/14756360701809910.
A series of 3-amino- and polyaminosterol analogues of squalamine and trodusquemine were synthesized and evaluated for their in vitro antimicrobial properties against human pathogens. The activity was highly dependent on the structure of the different compounds involved and the best results were obtained with aminosterol derivatives 4b, 4e, 8b, 8e and 8n exhibiting minimum inhibitory concentrations (MICs) against yeasts, Gram positive and Gram negative bacteria at average concentrations of 3.12-12.5 microM.
合成了一系列鲨胺和曲古抑菌素的3-氨基及多氨基甾醇类似物，并评估了它们对人类病原体的体外抗菌特性。活性高度依赖于所涉及的不同化合物的结构，氨基甾醇衍生物4b、4e、8b、8e和8n对酵母、革兰氏阳性菌和革兰氏阴性菌表现出最低抑菌浓度（MIC），平均浓度为3.12-12.5微摩尔，取得了最佳结果。
