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학술발표회초록보기

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  • 03월 02일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Construction of a Unique Drug-like 2,4,5-trisubstituted Thiazole Libraries Using BAL Resin on Solid-phase

등록일
2012년 2월 14일 19시 23분 29초
접수번호
0333
발표코드
MEDI.P-984 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 25일 (수요일) 18:00~21:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
배미선, 김용상, 유서현, 공영대
동국대학교 화학과, Korea
Among organic small molecules, heterocyclic compounds have received particular attention in combinatorial chemistry, since they are important structural components of bioactive molecules. In this regard, owing to the fact that thiazole derivatives exhibit a wide range of important biological activities, they serve as attractive targets for combinatorial library construction via solid-phase synthesis. For example, thiazoles exhibits the activities against cyclin-dependent kinase (CDK) and glycogen synthase kinase-3 (GSK-3). Herein we would like to present a novel solid-phase synthetic method for combinatorial generation of 2,4,5-trisubstituted thiazole derivatives through resin-bound BAL linker. We had previously report a useful method for the solid-phase synthesis of 2,4,5-trisubstituted thiazole derivatives using a sulfone traceless linker. However, the developed method some limitation which were couldn’t introduce efficiently various substitutents such as amine, amides, sulfone amides, and urea on the 2-position of thiazole core skeleton by nucleophilic substitution reaction at last cleavage step. We are studying cleavage condition on solid-support under TFA. Therefore, we believe our efficient approach is suitable for the construction of drug-like 2,4,5-trisubstituted thiazole libraries in a high throughput manner.

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