Direct Synthesis of N-Functionalized Dipropargylamine Linkers as Models for Use in Peptide Stapling

被引:0
作者
Renzetti, Andrea [1 ]
Rutherford, Ryan N. [2 ]
Fukumoto, Kozo [3 ]
Kunciw, Dominique [1 ]
Sore, Hannah F. [1 ]
Spring, David R. [1 ]
机构
[1] Univ Cambridge, Dept Chem, Lensfield Rd, Cambridge CB2 1EW, England
[2] Sci Educ Acad Ryukyus, 1 Senbaru, Nishihara, Okinawa 9030213, Japan
[3] Univ Ryukyus, Fac Educ, 1 Senbaru, Nishihara, Okinawa 9030213, Japan
基金
欧洲研究理事会; 英国工程与自然科学研究理事会; 英国生物技术与生命科学研究理事会; 日本科学技术振兴机构; 英国惠康基金;
关键词
peptides; stapling; linkers; amines; alkynes; click chemistry; ANTIMICROBIAL PEPTIDES; DRUG DESIGN; HELIX;
D O I
10.1055/s-0039-1690217
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
N-Substituted dipropargylamines that are suitable as functionalized linkers for peptide stapling can be synthesized in one step under mild conditions from commercially available starting materials (41% to quantitative yield).
引用
收藏
页码:2153 / 2156
页数:4
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