Atcher Joan, Solà Jordi, Alfonso Ignacio
Department of Biological Chemistry and Molecular Modelling, IQAC-CSIC, Jordi Girona, 18-26, 08034, Barcelona, Spain.
Org Biomol Chem. 2016 Dec 20;15(1):213-219. doi: 10.1039/c6ob02441f.
A straightforward four-step synthesis leads to the preparation of C-symmetric dithiols containing a central aromatic core and amino acid side chains. These building blocks allow the preparation of dynamic covalent libraries of pseudopeptidic macrocycles in aqueous media that cover a broad range of polarities, functional groups and bulkiness mirroring the diversity found in natural peptides. The versatility of the generated dynamic libraries has been illustrated by the amplification of two different members from the same library upon the action of two biologically relevant templates.
一种直接的四步合成法可用于制备含有中心芳香核和氨基酸侧链的 C 对称二硫醇。这些构建模块能够在水性介质中制备假肽大环的动态共价库,该库涵盖了广泛的极性、官能团和体积,反映了天然肽中存在的多样性。通过在两种生物学相关模板的作用下从同一库中扩增出两种不同的成员,证明了所生成的动态库的多功能性。