摘要
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.
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.
作者
黄净
杨毅华
冯娟
李军章
刘守信
Huang Jing;Yang Yihua;Feng Juan;Li Junzhang;Liu Shouxin(State Key Laboratory Breeding Base,Hebei Key Laboratory of Molecular Chemistry for Drug,Hebei University of Science&Technology,Shijiazhuang,Hebei 050018;College of Chemical and Pharmaceutical Engineering,Hebei University of Science&Technology,Shijiazhuang,Hebei 050018)
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2020年第6期1473-1483,共11页
Chinese Journal of Organic Chemistry
基金
“973”计划前期研究专项课题(Nos.2011CB512007,2012CB723501)
国家自然科学基金(Nos.30472074,30873139)资助项目。
