ヒグチ　ケイ   Higuchi Kei   樋口　慧    所属   東邦大学  薬学部 薬学科    職種   准教授
論文種別	原著
言語種別	英語
査読の有無	査読あり
表題	Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors.
掲載誌名	正式名：ACS medicinal chemistry letters
掲載区分	国外
巻・号・頁	9(9),pp.884-888
著者・共著者	Hiranaka S,Tega Y,Higuchi K,Kurosawa T,Deguchi Y,Arata M,Ito A,Yoshida M,Nagaoka Y,Sumiyoshi T
発行年月	2018/09
概要	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.
DOI	10.1021/acsmedchemlett.8b00099
PMID	30258535