期刊
ARCHIV DER PHARMAZIE
卷 351, 期 5, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201800018
关键词
annulated thienopyrimidines; cycloalkene-fused thienopyrimidines; phosphodiesterase inhibitor; planarity
资金
- National Cancer Institute (USA) [NCI 5 R01 CA155638]
Novel cycloalkene-fused thienopyrimidine analogues with enhanced phosphodiesterase 5 (PDE5) inhibitory properties are presented. The structure of the reported scaffold was modulated through variation of the terminal cycloalkene ring size, as well as by varying the substituents at position 4 through the attachment of different groups including aniline, benzylamine, cyclohexylethylamine, methyl/acetyl/aryl piperazines, and aryl hydrazones. Compound 15Y with a benzylamine substituent and cycloheptene as terminal ring showed the highest PDE5 inhibitory activity with an IC50 value as low as 190 nM and with good selectivity versus PDE7 and PDE9.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据