| 초록 |
Cyclic peptide has been to the fore as a privileged structure recently with excellent properties such as stability and membrane permeability. Cyclosporin A (CsA) and daptomycin are naturally occurring cyclic peptides, which demonstrated their versatile pharmacological activity such as immunosuppressant or antibacterial activity. Recent studies show peptidomimetic macrocycles demonostrated improved bioactivity and pharmacokinetic profiles compared to natural compound. Herein, a new class of peptide-peptoid hybrid macrocycle was designed. Basic scaffold was adopted from CsA, and peptoid residues, N-substituted glycines, substituted for some part of the cyclic peptide sequence at the β-turn positions. Macrocyclic peptide-peptoid hybrids were synthesized via standard SPPS, while cyclization was performed in a solution phase. Employing the framework of peptide-peptoid hybrid, molecular diversity can be achieved providing a library of privileged structures in the bRo5 chemical space. |
