Design, synthesis, and biological activity of certain quinazolinedione derivatives as potent phosphodiestrase4 inhibitors

被引：0
作者：
Afaf K. Elansary
Hanan H. Kadry
Eman M. Ahmed
Amr Sayed Motawi Sonousi
机构：
[1] Cairo University,Department of Organic Chemistry, Faculty of Pharmacy
来源：
Medicinal Chemistry Research | 2012年 / 21卷
关键词：
Synthesis; Phosphodiestase4B (PDE4b) inhibitor; Quinazolindiones; Docking study;
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学科分类号：
摘要：
In this study, a series of 3-butylquinazolinedione linked with different substituent to N1 of quinazoline nucleus have been synthesized. Some of the new final compounds tested in vitro for their inhibitory activity against phosphodiestrase 4B which is the enzyme responsible for the hydrolysis of cyclic adenosine mono phosphate, the second messenger involved in the regulation of important cell functions. Compound 7f (100%) showed inhibition better than rolipram (90%), while the other tested compounds showed moderate activity. Docking study has been done to rationalize the obtained biological results.
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页码：3557 / 3567
页数：10
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