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제118회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis of privileged Thiazolodiazepinones

등록일
2016년 8월 31일 14시 45분 22초
접수번호
2229
발표코드
MEDI.P-503 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 13일 (목요일) 11:00~12:30
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
김다현, 김주빈, 김소희, 이태호*
경북대학교 약학과, Korea
The 1,4-benzodiazepine scaffold is utilized a lot in medicinal chemistry. For example, diazepam well-known as a drug for anxiety treatment contains a 1,4-benzodiazepine. Also, a variety of benzodiazepine derivatives are reported they have many biological activities. These have shown activities as inhibition the proliferation of tumor cells, antitrypanosomal activity, γ-secretase inhibitor, histone deacetylase inhibitors (HDACi), the peptide hormone cholecystokinin (CCK) antagonist, anticancer agent and p53-HDM2 interaction antagonist. In addition, by acting on central nervous system as GABA receptor agonists, they could be applied to insomnia, trouble sleeping and convulsion. Thus, they serve as attractive scaffolds for combinatorial library construction via solution-phase synthesis. Herewith, we have tried to construct a small molecule library based thiazolodiazepinone via solution-phase parallel synthesis. The synthetic strategy includes directly amide bond formation of 2-aminothiazole with protected glycine. After the additional diverse moieties are introduced, nucleophillic substitution is achieved with various amine nucleophiles to give 2,4,6,8-tetrasubstituted-thiazolodiazepinone derivatives in good overall yield.

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