摘要/Abstract
介绍了环肽化合物中顺式（cis-）和反式（trans-）结构特点，分别针对不含N-取代的环肽、含脯氨酸残基的环肽以及含N-甲基化残基的天然环肽，讨论了cis-或trans-结构在上述环肽及结构类似物中的研究进展，以及这种cis-或trans-结构对环肽生物活性的潜在影响.脯氨酸由于其刚性吡咯环结构而显著影响着环肽分子构象，N-甲基化残基不仅增大了空间位阻，而且能够诱导增大酰胺键cis-结构比例.
关键词: cis-/trans-结构, cis-/trans-异构体, 环肽, 生物活性
This paper focuses on cis-/trans-conformational interchanges of amide bonds in cyclic peptides that contain N-unsubstituted amino acids, N-methylated amino acids, and prolines. Conformational preferences of such cyclic peptides and their analogs are discussed. Proline has strong influences on the conformation due to the five-membered cyclic structure. N-Methylation not only increased the steric hindrance, but also led to increased population of cis-conformation of the amide bond.
Key words: cis-/trans-structure, cis-/trans-isomerization, cyclic peptide, bioactivity
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