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

제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Solid-phase Synthesis of Drug-like 5-Phenyl-(2-amino and 2-amido substituted) 1,3,4-Oxadiazole Library via Reagent-based Cyclization of Thiosemicarbazide

등록일
2012년 2월 14일 19시 24분 39초
접수번호
0341
발표코드
MEDI.P-992 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 25일 (수요일) 18:00~21:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
양승주, 이석형, 곽세훈, 공영대
동국대학교 화학과, Korea
Solid-phase organic synthesis(SPOS) is now routinely used to prepare druglike, small organic molecules in medical chemistry programs. This procedure enables the generation of massive numbers of hit and lead compounds as part of high-throughput screening technologies. Heterocyclic compounds are commonly used scaffolds on which pharmacophores are arranged to provide potent and selective drugs. This is especially true for five-membered ring heterocyclic compounds, which serve as the core components of a large number of substances that posses a wide range of interesting biological activities. As a part of our ongoing drug discovery program, we have been exploring the potential of resin-bound 1,3,4-oxadiazole derivatives as a versatile intermediate for generation of drug-like heterocyclic compound libraries. The 2-amino 2-amido substituted 1,3,4-oxadiazole derivatives have attracted much attention for their interesting biological activities such as COX-2, 5-LO, and various receptor antagonistic. Herein we would like to present a novel solid-phase synthetic method for combinatorial generation of 1,3,4-oxadiazole library via reagent-based cyclization of thiosemicarbazide. The final compounds were obtained in good yields and high purities upon cleavage from the resins.

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