神经营养肽醛类：费卢他胺B及其简化类似物的固相合成
Neurotrophic peptide aldehydes: solid phase synthesis of fellutamide B and a simplified analog.
作者信息
Schneekloth John S, Sanders John L, Hines John, Crews Craig M
机构信息
Department of Molecular, Cellular, and Developmental Biology, Yale University, PO Box 208103, New Haven, CT 06520-8103, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jul 15;16(14):3855-8. doi: 10.1016/j.bmcl.2006.04.029. Epub 2006 May 11.
Abstract
A combination of solid phase and solution phase synthetic methods have been used to complete the total synthesis of the neurotrophic lipopeptide aldehyde fellutamide B (2). The beta-hydroxy aliphatic tail was prepared by regioselective reductive opening of a cyclic sulfate, and later coupled to a solid phase resin. The synthetic compound was then examined in cytotoxicity and nerve growth factor (NGF) induction assays. A simplified analog of fellutamide B also showed activity.
摘要
固相和溶液相合成方法相结合已用于完成神经营养脂肽醛类化合物费卢他胺B（2）的全合成。β-羟基脂肪族尾链通过环状硫酸酯的区域选择性还原开环制备，随后与固相树脂偶联。然后对合成化合物进行细胞毒性和神经生长因子（NGF）诱导试验检测。费卢他胺B的一种简化类似物也显示出活性。
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