Peptidomimetics have demonstrated biological activity toward a broad range of medicinal targets. Although aziridine containing peptidomimetics have been reported, there are no examples of N-acyl aziridines. We have recently shown that fused ring aziridines can be converted to aziridinyl ureas by reaction with amine nucleophiles. We will present new examples of this reaction using amino acids and peptides as the nucleophile to generate peptidomimetics containing an aziridinyl urea. Structural and biological studies with these novel peptidomimetics will also be presented.

Synthesis of N-acyl aziridine containing peptidomimetics

245th National Meeting (2013)

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