Preparation of Constrained Unnatural Aromatic Amino Acids via Unsaturated Diketopiperazine Intermediate |
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| Authors: | Adriano Mollica Roberto Costante Sako Mirzaie Simone Carradori Giorgia Macedonio Azzurra Stefanucci Ettore Novellino |
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| Institution: | 1. Dipartimento di Farmacia, Università di Chieti‐Pescara “G. d'Annunzio”, Chieti, Italy;2. Department of Biochemistry, Sanandaj Branch, Islamic Azad University, Sanandaj, Iran;3. Dipartimento di Chimica, Sapienza, Università di Roma, Rome, Italy;4. Dipartimento di Farmacia, Università di Napoli “Federico II”, Naples, Italy |
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| Abstract: | Unnatural aromatic amino acids are useful tools in drug discovery, since their insertion in bioactive peptide sequences can change the side chains spatial orientation, the backbone conformation and above all, their bioactivity. In this communication, we propose a straightforward method to synthesize 2′,6′‐dimethyl‐tyrosine and 2′,6′‐dimehylphenyl‐alanine derivatives as handling building blocks for peptide synthesis via unsaturated diketopiperazine (DKP) intermediate. |
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