|
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 |
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