Synthesis of Dehydroamino Acids and Their Applications in the Drug Research and Development
Tong Wang , Wenjiao Zhao , Liangchun Li , Renlin Zheng , Dequn Sun
Progress in Chemistry ›› 2020, Vol. 32 ›› Issue (1) : 55 -71.
Traditional polypeptides usually have the disadvantages of easy hydrolyzation, poor cell membrane permeability, and unstable conformation, which limits their application as a drug in the field of disease treatment. The conformational restriction caused by incorporation of dehydroamino acids into polypeptide can effectively improve the metabolic stability and bioavailability of peptides. In this paper, the synthesis methods and the recent applications in drug design of four kinds of dehydroamino acids including α,β-dehydro-α-amino acids, β,γ-dehydro-α-amino acids, α-dehydro-β-amino acids and α,β-dehydro-β-amino acids are reviewed, which could provide reference for the related research.
dehydroamino acids / peptidomimetics / conformational restriction / synthesis / drug design
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