Salmi Chanaz, Loncle Celine, Vidal Nicolas, Letourneux Yves, Brunel Jean Michel
Laboratoire SESNAB, Biosciences, UMR-MD-1, case 342, Faculté de St Jérôme, Université Paul Cézanne, Av. Escadrille Normandie Niemen, 13397 Marseille, Cedex 20, France.
Eur J Med Chem. 2008 Mar;43(3):540-7. doi: 10.1016/j.ejmech.2007.04.006. Epub 2007 May 5.
A series of 3-amino and polyaminosterol analogues of squalamine and trodusquemine were synthesized involving a new stereoselective titanium reductive amination reaction in high chemical yields of up to 95% in numerous cases. These derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. Activity was highly dependent on the different compounds' structures involved and best results have been obtained with aminosterol derivatives 4b, 4e and 6i exhibiting activities against yeasts, Gram positive and Gram negative bacteria at average concentrations of 6.25-12.5 microg/mL.
合成了一系列角鲨胺和曲古抑菌素的3-氨基及多氨基甾醇类似物，其中涉及一种新的立体选择性钛还原胺化反应，在许多情况下化学产率高达95%。对这些衍生物针对人类病原体的体外抗菌特性进行了评估。活性高度依赖于所涉及的不同化合物结构，氨基甾醇衍生物4b、4e和6i表现出对酵母、革兰氏阳性菌和革兰氏阴性菌的活性，平均浓度为6.25 - 12.5微克/毫升，取得了最佳结果。
