Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 민선준 | - |
dc.date.accessioned | 2019-05-07T02:45:01Z | - |
dc.date.available | 2019-05-07T02:45:01Z | - |
dc.date.issued | 2017-07 | - |
dc.identifier.citation | ACS CHEMICAL NEUROSCIENCE, v. 8, No. 7, Page. 1519-1529 | en_US |
dc.identifier.issn | 1948-7193 | - |
dc.identifier.uri | https://pubs.acs.org/doi/abs/10.1021/acschemneuro.7b00050 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/103464 | - |
dc.description.abstract | To develop novel, selective, and reversible MAO-B inhibitors for safer treatment of Parkinson's disease, benzothiazole and benzoxazole derivatives with indole moiety were designed and synthesized. Most of the synthesized compounds showed inhibitory activities against MAO-B and selectivity over MAO-A. The most active compound was compound 5b, 6-fluoro-2-(1-methyl-IN-indol-5-yl)benzo[d]-thiazole with an IC50 value of 28 nM with no apparent effect on MAO-A activity at 10 mu M. Based on the reversibility assay, compound 5b turned out to be fully reversible with over 95% of recovery of enzyme activity after washout of the compound. Compound Sb showed a reasonable stability in human liver microsomes and did not affect the activities of CYP isozymes, suggesting an absence of high-risk drug-drug interaction. In an in vivo MPTP-induced animal model of Parkinson's disease, oral administration of compound 5b showed neuroprotection of nigrostriatal dopaminergic neurons as revealed by tyrosine hydroxylase staining and prevention of MPTP-induced parkinsonism as revealed by motor behavioral assay of vertical grid test. In summary, the novel, reversible, and selective MAO-B inhibitor compound 5b was synthesized and characterized. We propose compound 5b as an effective therapeutic compound for relieving parkinsonism. | en_US |
dc.description.sponsorship | This work was supported by the Korea Institute of Science and Technology (KIST) Institutional Program (2E26850) and the Original Technology Research Program (NRF-2016M3C7A1904344) funded by the National Research Foundation of Korea (NRF). | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | AMER CHEMICAL SOC | en_US |
dc.subject | benzothiazole | en_US |
dc.subject | benzoxazole | en_US |
dc.subject | MAO-B | en_US |
dc.subject | MAO-B inhibitor | en_US |
dc.subject | MPTP-induced animal model | en_US |
dc.subject | Parkinson's disease | en_US |
dc.title | Indole-Substituted Benzothiazoles and Benzoxazoles as Selective and Reversible MAO-B Inhibitors for Treatment of Parkinson's Disease | en_US |
dc.type | Article | en_US |
dc.relation.no | 7 | - |
dc.relation.volume | 8 | - |
dc.identifier.doi | 10.1021/acschemneuro.7b00050 | - |
dc.relation.page | 1519-1529 | - |
dc.relation.journal | ACS CHEMICAL NEUROSCIENCE | - |
dc.contributor.googleauthor | Nam, Min-Ho | - |
dc.contributor.googleauthor | Park, Moosung | - |
dc.contributor.googleauthor | Park, Hyeri | - |
dc.contributor.googleauthor | Kim, Youngjae | - |
dc.contributor.googleauthor | Yoon, Seulki | - |
dc.contributor.googleauthor | Sawant, Vikram Shahaji | - |
dc.contributor.googleauthor | Cho, Ji Won | - |
dc.contributor.googleauthor | Park, Jong-Hyun | - |
dc.contributor.googleauthor | Park, Ki Duk | - |
dc.contributor.googleauthor | Min, Sun-Joon | - |
dc.contributor.googleauthor | Lee, C. Justin | - |
dc.contributor.googleauthor | Chooaii, Hyunah | - |
dc.relation.code | 2017011526 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E] | - |
dc.sector.department | DEPARTMENT OF CHEMICAL AND MOLECULAR ENGINEERING | - |
dc.identifier.pid | sjmin | - |
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