Synthesis of a 24-membered cyclic peptide-biphenyl hybrid

被引:17
作者
Montero, Ana
Albericio, Fernando
Royo, Miriam
Herradon, Bernardo
机构
[1] CSIC, Inst Quim Organ Gen, E-28006 Madrid, Spain
[2] Univ Barcelona, Combinatorial Chem Unit, E-08028 Barcelona, Spain
[3] Univ Barcelona, Inst Res Biomed, E-08028 Barcelona, Spain
[4] Univ Barcelona, Dept Organ Chem, E-08028 Barcelona, Spain
关键词
biaryls; calpain inhibitors; macrocycles; peptide-biphenyl hybrids; solid-phase synthesis;
D O I
10.1002/ejoc.200600833
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of a 24-membered macrocyclic peptide-biphenyl hybrid with four amino acid residues and two biphenyl fragments was performed by a combination of solid-phase and solution methodologies. The acyclic precursor was prepared by a solid phase methodology whereas the final macrocyclization was carried out by diisopropylcarbodiimide (DIPCDI) and N-hydroxybenzotriazole (HOBt) in solution. The target molecule was a moderate inhibitor of p-calpain. ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007).
引用
收藏
页码:1301 / 1308
页数:8
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