期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 9, 期 9, 页码 884-888出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00099
关键词
Histone deacetylase; HDAC inhibitor; blood-brain barrier; selective inhibitor; pyrilamine-sensitive proton-coupled organic cation antiporter
资金
- Kansai University
- JSPS KAKENHI [JP15K18903]
- MEXT-Supported Program for the Strategic Research Foundation at Private Universities (2013-2017), Japan
We designed and synthesized a pyrilamine derivative 1 as a selective class I HDAC inhibitor that targets pyrilamine-sensitive proton-coupled organic cation antiporter (PYSOCA) at the blood-brain barrier (BBB). Introduction of pyrilamine moiety to benzamide type HDAC inhibitors kept selective class I HDAC inhibitory activity and increased BBB permeability. Our BBB transport study showed that compound 1 is a substrate of PYSOCA. Thus, our findings suggest that the hybrid method of HDAC inhibitor and substrate of PYSOCA such as pyrilamine is useful for development of HDAC inhibitors with increased BBB permeability.
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