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  • 02월 19일 23시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제119회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Benzo[d]oxazole derivatives as selective MAO-B inhibitors for treatment of Parkinson’s disease

등록일
2017년 2월 16일 14시 19분 52초
접수번호
4410
발표코드
MEDI.P-461 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 20일 (목요일) 11:00~12:30
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
Vikram Shahaji Sawant, 추현아1,*
한국과학기술연구원(KIST) 뇌의약연구단, Korea
1한국과학기술연구원(KIST) 생명보건본부, Korea
Parkinson’s disease is the second most common neurodegenerative disease in developed countries after Alzheimer's disease. Monoamine oxidase B as a mitochondrial bound enzyme is involved in catabolic oxidative deamination of dopamine. As the increased levels of MAO-B result in death of dopaminergic neurons in substantia nigra, MAO-B is considered as potential target for treating Parkinson’s disease. As a part of our continuous search for selective MAO-B inhibitors, a series of benzo[d]oxazoles are synthesized and structure-activity relationship (SAR) study was carried out. Among the synthesized benzo[d]oxazole compounds, compounds 8f and 8e are the most active compounds with IC50 values of 58.9 nM and 68.5 nM, respectively, which showed selectivity over MAO-A. We also performed the molecular docking study for the investigation of the binding mode of novel MAO-B inhibitors.

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