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

제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Solid-phase Parallel Synthesis of a Novel N-[Alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted Amide and Amine Drug-like Libraries

등록일
2012년 2월 14일 19시 23분 43초
접수번호
0336
발표코드
MEDI.P-987 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 25일 (수요일) 18:00~21:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
김지혜, 이지형, 김슬기, 공영대
동국대학교 화학과, Korea
Over several years, we have investigated many structural classes of 5-LO inhibitors with the aim of identifying orally active 5-LO (5-lipoxygenase) target as anti-inflammatory inhibitors. As the results, we found out a novel 6-amino-2,2-dimethyl-3,4,6-trisubstituted-2H-1-benzopyran hit compound (one representative lead compound is KRH-102140 with the 6-amino-2,2-dimethyl-3,4,6-trisubstituted-2H-1-benzopyran and showed good in vitro activity at 0.16 ?m IC50 value)4a toward 5-LO target.4 However, we didn’t find out much improved hit compound by optimization process of KRH-102140 core skeleton derivatives. Therefore, our concern focused on the development of a spiro-benzopyran core skeleton to improve more active benzopyran derivatives then the KRH-2140. As the results, we report a solid-phase parallel synthesis of a novel N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B derivatives that relies on BAL linker and present an chemical properties using a in silico screening.

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