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  • 09월 05일 13시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

Design, Synthesis and Biological Evaluation of Piperazine and Piperidine Analogues as CB1 Cannabinoid Receptor Ligands

등록일
2007년 8월 1일 14시 18분 43초
접수번호
0013
발표코드
35P260포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 <발표Ⅱ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
송광섭, 김종엽, 김정민, 장종환, 이진화
(주)녹십자 종합연구소,
After the CB1 receptor antagonist SR141716 (rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target in the treatment of obesity. Several series of derivatives based on 1-benzhydrylpiperazine and 1-benzhydrylpiperidine scaffold were synthesized and tested for CB1 receptor binding affinity. These derivatives have 1-benzhydrylpiperazine or 1-benzhydrylpiperidine combined with the various moieties, such as urea, carbamate, amide, sulfonamide and oxalamide. The SAR study to optimize the CB1 binding affinity led to the potent urea derivatives. Through the further SAR study to optimize the substituents of diphenyl ring, the combination of 2-chlorophenyl and 4-chlorophenyl turned out to be the most potent scaffold. This study introduces several novel CB1 antagonists with IC50 < 100 nM for the CB1 receptor binding. The CB2 binding affinity was assessed in order to determine CB2/CB1 selectivity and the functional profiles of several compounds were also evaluated by CRE-luciferase assay.

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