Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings
Zhou Zhong-Zhen
Ge Bing-Chen
Zhong Qiu-Ping
Huang Chang
Cheng Yu-Fang
Yang Xue-Mei
Wang Hai-Tao
Xu Jiang-Ping
· 2016
期刊名称：
European Journal of Medicinal Chemistry
2016 年
124 卷
摘要：
In this study, catecholamides (7a??“l) bearing different aromatic rings (such as pyridine-2-yl, pyridine-3-yl, phenyl, and 2-chlorophenyl groups) were synthesized as potent phosphodiesterase (PDE) 4 inhibitors. The inhibitory activities of these compounds were evaluated against the core catalytic domains of human PDE4 (PDE4CAT), full-length PDE4A4, PDE4B1, PDE4C1, and PDE4D7 enzymes, and other PDE family members. Eight of the synthesized compounds were identified as having submicromolar IC
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