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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-626 |
| Subject |
Construction of Thiazolopyrimidinone using Solid-phase Synthesis |
| Authors |
YunJi Jin, GeunHyung Jo, Taeho Lee1,*
Kyungpook National University, Korea
1Department of Pharmacy, Kyungpook National University, Korea
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| Abstract |
Combinatorial chemistry play an important role in the area of drug discovery process and medicinal chemistry. In the chemistry, Solid-phase organic synthesis is a method in which generate chemical library and necessary to search of drug-like compound. Through this method, we have studied about the construction of heterocyclic compounds because heterocyclic compounds serve as key structural component of bioactive molecules. In this study, we have an interested in heterocyclic compound containing thiazolopyrimidinone moiety. The substituted thiazolopyrimidinone derivatives are a useful scaffold found in wide range of important biological activities. For example, GHS-R1a antagonists and inverse agonists for the treatment of obesity, selective Pl3K-beta inhibitors, anti-tumor EGFR tyrosine kinase inhibitors, melanin-concentrating hormone receptor 1(MCH R1) antagonists. In addition, thiazolopyrimidinone derivatives reported to exhibit antiviral, antimicrobial, neurotropic, antihistaminic, antihypertensive and analgesic. Thus the thiazolopyrimidinone and fused-thiazolopyrimidinone heterocycles are important structural components of biological activities, and, as a result, it is necessary to build the thiazolopyrimidinone derivatives library by way of solid-phase synthesis. Synthesis of these derivatives was carried out using Merrifield resin, which is a solid support, after alkylation, cyclization and oxidation, reacted with various nucleophiles to finally obtain thiazole-fused ring derivatives with good purity and yield. |
| E-mail |
yundzzang@naver.com |
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121st General Meeting of the KCS