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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-303 |
| Subject |
Solid-Phase Parallel Synthesis of a 1,3,4-Oxadiazole Based β-Turn Mimetic Library |
| Authors |
AIZHAN ABDILDINOVA, seung ju yang, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
|
| Abstract |
Β-turn is a protein secondary structure element and known to be modulating protein-protein interactions. 1,3,4-oxadiazole derivatives also known to have a wide range of biological activities such as anticancer, antibacterial, antimicrobial, anti-inflammatory, etc. Combination of a small molecule fragment with peptide motif can improve pharmacokinetic properties of both peptide and small molecule and provide more effective drug probes. In this study, we developed an efficient and mild method for the synthesis of α-amino acid substituted 1,3,4-oxadiazoles that mimic the bioactive β-turn structural motif of proteins. Initial synthesis starts from the reaction between thiosemicarbazide resin with α-amino acid and further cyclization to the 1,3,4-oxadiazole. Further functionalization with adding more α-amino acids for the chain prolongation and cleavage from the supporting resin can provide library of desired β-turn mimetic compounds. |
| E-mail |
aizhik.a91@gmail.com |
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120th General Meeting of the KCS