| 摘要 |
The invention relates to the field of candidate drug testing and drug development. A method is provided for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule capable of reacting with the at least first and second reactive group; contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the at least one molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage, preferably wherein the coupling reaction is performed in solution, more preferably in an aqueous solution. Furthermore, a method is provided for selecting a candidate drug compound comprising providing a library of compounds according to the invention and determining the binding of a target molecule to the compounds. |
| 主权项 |
1. A method for synthesizing a compound comprising at least one peptide structure attached via at least two thioether linkages to a (hetero)aromatic molecule, the method comprising:
providing a (hetero)aromatic molecule comprising a bis-, tris-, or tetrakis(halomethyl)-substituted (hetero)aromatic ring system; providing at least one peptide comprising at least one amino acid having a side chain comprising an unprotected functional group selected from the group consisting of amine, guanidinium, amido, carboxylic acid, alcohol, phenol, indole, thioether, and imidazole, wherein the peptide further comprises at least two SH functionalities; and contacting the (hetero)aromatic molecule and the at least one peptide in a buffered aqueous solution comprising at least 50% water, to form in a coupling reaction the compound comprising at least one peptide structure attached via at least two thioether linkages to the (hetero)aromatic molecule, wherein each of the thioether linkages is formed between one of the halomethyl substituents on the (hetero)aromatic ring system and one of the SH functionalities.
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