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Synthesis of pyridazine-based scaffolds as alpha-helix mimetics
Alessandro Volonterio1, Lionel Moisan, Julius Rebek
1The Skaggs Institute for Chemical Biology and Department of Chemistry, The Scripps Research Institute MB-26, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
Abstract:
The synthesis of several amphiphilic, nonpeptidic scaffolds that mimic the presentation of i, i + 3 or i + 4, and i + 7 residues of a peptide alpha-helix is described. The approach uses a pyridazine core, and the synthesis involves only a few steps and minimizes the number of C-C bond-forming reactions. The versatility of the synthesis makes it suitable for the preparation of small libraries of low molecular weight alpha-helix mimetics that could be targeted to certain protein/protein interactions.
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