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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Grand Ballroom |
| Time |
10월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-307 |
| Subject |
Design and Solid-Phase Parallel Synthesis of 2,4,5-Trisubstituted Thiazole Derivatives as a Potential Sphingosylphosphorylcholine (SPC) Receptor Inhibitors |
| Authors |
Hyejin Kwon, Sun Hwa Jung, Young Dae Gong*
Department of Chemistry, Dongguk University, Korea
|
| Abstract |
In this study, we prepared library of 2,4,5-trisubstituted thiazole derivatives via solid-phase synthesis by introducing various electrophile substituents such as acyl halide, alkyl hlide to the 2,4-diamino(thiazole-5-yl)substituted-phenylmethanone resin. We are expecting that synthesized 2,4,5-trisubstituted thiazole derivatives will show biological activity against SPC receptor because 2,4-disubstituted-5 aminocarbonyl-1,3-thiazole derivatives is already known as a good therapeutic agent toward SPC. SPC plays a multifunctional role such as cell growth, differentiation, calcium signaling, tissue remodeling. Prominent skin disorders, such as psoriasis and atopic dermatitis, have diminished epidermal ceramide levels, reflecting altered SPC metabolism.
In previous studies, the sulfone traceless linker was introduced to the Merrifield resin for the synthesis of 2,4,5-trisubstituted thiazole derivatives. However, this methodology only can give diversity to 2,4-diamino(thiazole-5-yl)substituted-phenylmethanone resin using nucleophile substituents. To improve the diversity of compounds, we have decided to introduce new carbamimidothioate linker to the Merrifield resin thus linker will act as a nucleophile and allow to introduce various electrophile substituents. As a result, an improved molecular diversity of the 2,4,5-trisubstituted thiazole library can serve more effectively in the development of a potential SPC receptor inhibitors. |
| E-mail |
khgin@hanmail.net |
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122nd General Meeting of the KCS