119th General Meeting of the KCS

Type Poster Presentation
Area 의약화학
Room No. 포스터발표장
Time 4월 20일 (목요일) 11:00~12:30
Code MEDI.P-461
Subject Benzo[d]oxazole derivatives as selective MAO-B inhibitors for treatment of Parkinson’s disease
Authors Vikram Shahaji Sawant, 추현아1,*
한국과학기술연구원(KIST) 뇌의약연구단, Korea
1한국과학기술연구원(KIST) 생명보건본부, Korea
Abstract 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.
E-mail 614513@kist.re.kr