Synthesis of New 3,20-Bispolyaminosteroid Squalamine Analogues and Evaluation of Their Antimicrobial Activities
Synthesis of New 3,20-Bispolyaminosteroid Squalamine Analogues and Evaluation of Their Antimicrobial Activities
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DOI：
10.1021/jm200506x
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发表时间：
2011-10-27
影响因子：
7.3
通讯作者：
Brunel, Jean Michel
中科院分区：
文献类型：
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作者：
Djouhri-Bouktab, Lamia;Vidal, Nicolas;Brunel, Jean Michel
角鲨胺和曲杜斯奎明的3，20-氨基和多氨基类固醇类似物的合成涉及立体选择性钛还原胺化反应，在许多情况下以高化学产率。评价这些衍生物对参比菌株和临床菌株的体外抗微生物性能，其最小抑菌浓度为2.5-40 μ g/mL。这些衍生物的作用机制，确定使用生物发光ATP流出测量和荧光方法膜去极化测定。
3,20-Amino- and polyaminosteroid analogues of squalamine and trodusquemine were synthesized involving a stereoselective titanium reductive amination reaction in high chemical yields in numerous cases. These derivatives were evaluated for their in vitro antimicrobial properties against references and clinical bacterial strains exhibiting minimum inhibitory concentrations of 2.5-40 mu g/mL. The mechanism of action of these derivatives was determined using bioluminescence for ATP efflux measurements and fluorescence methods for membrane depolarization assays.