硫醚
化学
二硫键
硫醇
催产素
神经肽
组合化学
肽
点击化学
立体化学
有机化学
生物化学
内科学
受体
医学
作者
Mark D. Nolan,Conor Shine,Eoin M. Scanlan,Rita Petracca
摘要
Disulfide bonds are an essential feature of many bioactive peptides, however, they are labile to reducing conditions which can limit therapeutic application. Herein, we report an efficient methodology for peptide macrocyclisation, furnishing thioether mimetics of disulfide linkages via thiol-ene click chemistry. Furthermore, this methodology is applied to the efficient synthesis of analogues of the neuropeptide oxytocin and in a highly efficient route to the clinical therapeutic carbetocin.
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