Molecules 2010-07-01

Solid-phase synthetic route to multiple derivatives of a fundamental peptide unit.

William L Scott, Ziniu Zhou, Paweł Zajdel, Maciej Pawłowski, Martin J O'Donnell

Index: Molecules 15(7) , 4961-83, (2010)

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Abstract

Amino acids are Nature's combinatorial building blocks. When substituted on both the amino and carboxyl sides they become the basic scaffold present in all peptides and proteins. We report a solid-phase synthetic route to large combinatorial variations of this fundamental scaffold, extending the variety of substituted biomimetic molecules available to successfully implement the Distributed Drug Discovery (D3) project. In a single solid-phase sequence, compatible with basic amine substituents, three-point variation is performed at the amino acid a-carbon and the amino and carboxyl functionalities.