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An Overview of the Synthesis of Biologically Active Cyclodepsipeptides

机译:概述生物活性环肽肽的合成

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Cyclodepsipeptide are a class of natural cyclic peptides that have a wide range of biological activities,hence the potential to be developed as new drug candidates.Cyclodpesipeptides comprise a backbone of amide bonds and at least one ester moiety,thus are complex and challenging to synthesis.Generally,cyclodepsipeptides are synthesised via solid-phase peptide synthesis,solution-phase or a combination of solid and solution-phase.Currently,solid-phase peptide synthesis is more in demand,but it also has several challenges in its application especially for the cyclodepsipeptide that contains N-methylated residues,as well as solution-phase peptide synthesis tends to have a longer reaction step.Therefore,the combination of solid and solution-phase peptide synthesis is a better alternative.This review discusses the synthetic strategies for cyclodepsipeptides including the preparation of precursor and macrocyclization.
机译:环肽甲基肽是一类天然环状肽,它们具有广泛的生物学活性,因此有可能作为新药候选物发育。环肽甲基肽包含酰胺键的骨干和至少一个酯部分的骨架,因此是复杂的,对合成而言是复杂的。 通常,通过固相肽合成,溶液或固体和溶液和溶液和溶液和溶液和溶液和溶液和溶液和溶液相结合,固相肽合成。固定相肽的合成更多,但它在其应用中尤其有一些挑战,尤其是对环肽肽的应用,固相和溶液相合成。 包含N-甲基化残基以及溶液相肽的合成往往具有更长的反应步骤。因此,固体和溶液和溶液相合成的组合是一种更好的替代方案。此评论讨论了包括环肽肽在内的综合策略 前体和大环化的制备。

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