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首页> 外文期刊>Journal of Medicinal Chemistry >Antileishmanial Ring-Substituted Ether Phospholipids
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Antileishmanial Ring-Substituted Ether Phospholipids

机译：抗leishmanial环取代的醚磷脂

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Three series of ring-substituted ether phospholipids were synthesized carrying N,N,N-trimethylammonium, N-methylpiperidino, or N-methylmorpholino headgroups. The first series is substituted by 2-cyclohexyloxyethyl or 2-(4-alkylidenecyclohexyloxy)ethyl groups, the second series by cyclohexylidenealkyl or adamantylidenealkyl moieties, and the third series by 2-aryloxyethyl or 6-aryloxyhexyl groups in the alkyl portion of the molecule. The antileishmanial activity of the new compounds was evaluated in vitro against the promastigote forms of L. donovani and L. infantum using an MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)-based microassay as a marker of cell viability. Analogues 12, 15, 24, 30, 32, 41, 43, and 45 were more potent than the control compound miltefosine (hexadecyulphosphocholine) against both L. donovani and L. infantum while, derivatives 13 and 42 were equipotent to miltefosine. Analogues 16, 17, 19, 20 were more potent than miltefosine against L. infantum and compounds 27, 31, 44 were more active than miltefosine against L. donovani. Differential scanning calorimetry (DSC) was used to probe the role of individual ether phospholipids on the physiochemical properties of model membranes. The DSC scans showed that the active compounds have a more profound effect on the thermotropic properties of model membrane bilayers than the less active ones.
机译：合成了带有N，N，N-三甲基铵，N-甲基哌啶子基或N-甲基吗啉代头基的三个系列的环取代的醚磷脂。第一个系列被分子的烷基部分中的2-环己基氧基乙基或2-（4-亚烷基亚环己基氧基）乙基取代，第二个系列被环己叉基烷基或金刚烷基烷基部分取代，而第三个系列被2-芳氧基乙基或6-芳基氧基己基取代。使用基于MTT（3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四唑鎓）的化合物在体外评估新化合物对抗多诺尼乳杆菌和婴儿乳杆菌的前鞭毛体形式的抗疟疾活性。微量测定作为细胞活力的标志。类似物12、15、24、30、32、41、43和45的抗药性比对照化合物miltefosine（十六烷基磷酸胆碱）对多诺氏乳杆菌和婴儿乳杆菌都有效，而衍生物13和42与miltefosine等价。类似物16、17、19、20比米非福星对婴儿乳杆菌更有效，化合物27、31、44的活性比米非福星对donovani乳杆菌更有效。差示扫描量热法（DSC）用于探究单个醚磷脂对模型膜理化性质的作用。 DSC扫描显示，活性化合物对模型膜双层的热致性影响要比活性较低的双层更深。

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