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|
| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2+3 |
| Time |
10월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-300 |
| Subject |
On-resin Cyclic Peptide Synthesis
via Cysteine side chain anchoring Pyroacm resin |
| Authors |
KangTae Kim, Young Dae Gong*, Vinayak Juvekar
Department of Chemistry, Dongguk University, Korea
|
| Abstract |
Cyclic peptides are regarded as important synthetic compounds because of their various biological activity. The constraint imposed from cyclization leads to enhancing biological activity as well as increasing resistance to proteolysis compared with linear peptides. Various lengths of cyclic peptides are synthesized to improve well-known cyclization method’s weakness using Pyroacm linker. The process involves initial immobilization of cysteine into pyroacm resin under acidic condition to avoid racemization. The β-elimination during peptide elongation controlled by using bulky protecting group at C-terminal. After elongation of peptide of required size, various on-resin cyclization processes have been screened. Peptides of smaller length showed both cyclization and homodimerization whereas peptide of six to seven amino acid residue, homodimerization was minimal. The process has been utilized to synthesis various cyclic peptide library containing four to seven amino acid residues. |
| E-mail |
kam1004@naver.com |
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120th General Meeting of the KCS