Basic techniques of working on a solid phase: From ABC of the peptide synthesis to libraries of non-natural amino acids

Basic techniques of working on a solid phase: From ABC of the peptide synthesis to libraries of non-natural amino acids
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DOI:
10.1134/s107036321012025x
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发表时间:
2010-12-01
影响因子:
0.9
通讯作者:
Ermolat'ev, D. S.
Ermolat'ev, D. S.
中科院分区:
化学4区
文献类型:
--
作者:
Babaev, E. V.;Ermolat'ev, D. S.

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在氨基上带有杂芳环(2-嘧啶基,取代的2-吡啶基或2-噻唑基)的几乎不可用的氨基酸库使用固相合成在各种树脂上制备。合成的化合物在结构上与一些已知的抗糖尿病药物相似。本文结合了综述的特点(对初学者的固相合成方法和技术的初步介绍,以及肽化学的选定方法)和作为方法工具有用的分步实验方案(由作者测试)。所提出的协议(固定化和修改的氨基酸,放置和删除的共同保护基团)不需要复杂的设备,并可能是有用的学生教育的图形介绍任务。
Libraries of hardly available amino acids bearing a heteroaromatic ring (2-pyrimidyl, substituted 2-pyridyl or 2-thiazolyl) at the amino group were prepared using solid-phase synthesis on various resins. The synthesized compounds are structurally similar to some known antidiabetic drugs. The paper combines features of a review (elementary introduction to the solid-phase synthesis methodology and technique for beginners and selected methods from peptide chemistry) and step-by-step experimental protocols (tested by the authors) useful as a methodic tool. The presented protocols (immobilization and modification of amino acids, placing and removal of common protective groups) require no sophisticated equipment and may be useful as pictorial introductory tasks for students education.